Sorafenib

别名: NSC-724772,BAY 43-9006 中文名称：索拉非尼

目录号：S7397 Purity: 99.89%

Sorafenib是Raf-1和B-Raf的多重激酶抑制剂，无细胞试验中IC50分别为6 nM和22 nM。Sorafenib 还可抑制VEGFR-2、VEGFR-3、PDGFR-β、Flt-3和c-KIT，对应的IC50值分别为90 nM、20 nM、57 nM、59 nM和68 nM。Sorafenib 可诱导autophagy、apoptosis并激活ferroptosis，Sorafenib 具有抗肿瘤活性。

Sorafenib Chemical Structure

CAS: 284461-73-0

规格	价格	库存
10mM (1mL in DMSO)	647.05	现货
20mg	573.93	现货
50mg	1040.95	现货
200mg	1392.3	现货
1g	4013.1	现货
2g	6306.3	现货
更大包装有超大折扣
400-668-6834 info@selleck.cn

产品质控

批次：纯度： 99.89%

99.89

Sorafenib相关产品

相关靶点	C-Raf/Raf-1 B-Raf A-raf	点击展开
相关产品	PLX-4720 LY3009120 AZ 628 GDC-0879 SB590885 TAK-632 RAF265 (CHIR-265) GW5074 Avutometinib PLX7904 Plixorafenib (PLX8394) ZM 336372 Tovorafenib (MLN2480) Agerafenib (CEP-32496) Lifirafenib (BGB-283) Naporafenib (LXH254) Belvarafenib RAF709 B-Raf inhibitor 1 (Compound 13) dihydrochloride CCT196969	点击展开
相关化合物库	激酶抑制剂库 MAPK抑制剂库细胞周期化合物库 TGF-beta/Smad信号通路库抗阿尔茨海默病化合物库	点击展开

细胞实验数据示例

细胞系	实验类型	活性描述	文献信息(PMID)
OS-RC-2	Growth Inhibition Assay	IC50=9.11243 μM	SANGER
LC-1F	Growth Inhibition Assay	IC50=9.10834 μM	SANGER
TE-10	Growth Inhibition Assay	IC50=8.76353 μM	SANGER
HD-MY-Z	Growth Inhibition Assay	IC50=8.63746 μM	SANGER
NB14	Growth Inhibition Assay	IC50=8.63133 μM	SANGER
IST-MEL1	Growth Inhibition Assay	IC50=8.40002 μM	SANGER
RPMI-8226	Growth Inhibition Assay	IC50=7.84511 μM	SANGER
ES8	Growth Inhibition Assay	IC50=7.76503 μM	SANGER
D-392MG	Growth Inhibition Assay	IC50=7.62663 μM	SANGER
NB1	Growth Inhibition Assay	IC50=7.40407 μM	SANGER
697	Growth Inhibition Assay	IC50=7.05989 μM	SANGER
DOHH-2	Growth Inhibition Assay	IC50=7.05676 μM	SANGER
SIMA	Growth Inhibition Assay	IC50=7.00101 μM	SANGER
OCI-AML2	Growth Inhibition Assay	IC50=6.61062 μM	SANGER
ML-2	Growth Inhibition Assay	IC50=6.52849 μM	SANGER
SW954	Growth Inhibition Assay	IC50=6.45866 μM	SANGER
MZ2-MEL	Growth Inhibition Assay	IC50=6.31839 μM	SANGER
MOLT-16	Growth Inhibition Assay	IC50=6.25266 μM	SANGER
SR	Growth Inhibition Assay	IC50=6.00678 μM	SANGER
BV-173	Growth Inhibition Assay	IC50=5.95682 μM	SANGER
no-11	Growth Inhibition Assay	IC50=5.73568 μM	SANGER
JAR	Growth Inhibition Assay	IC50=5.50824 μM	SANGER
NCI-H510A	Growth Inhibition Assay	IC50=5.41685 μM	SANGER
TE-12	Growth Inhibition Assay	IC50=5.24929 μM	SANGER
SF539	Growth Inhibition Assay	IC50=5.13227 μM	SANGER
QIMR-WIL	Growth Inhibition Assay	IC50=5.07294 μM	SANGER
NOMO-1	Growth Inhibition Assay	IC50=4.48905 μM	SANGER
MHH-PREB-1	Growth Inhibition Assay	IC50=4.40484 μM	SANGER
NCI-H1581	Growth Inhibition Assay	IC50=4.28798 μM	SANGER
BC-3	Growth Inhibition Assay	IC50=4.23391 μM	SANGER
SK-NEP-1	Growth Inhibition Assay	IC50=4.16815 μM	SANGER
KS-1	Growth Inhibition Assay	IC50=3.88198 μM	SANGER
ST486	Growth Inhibition Assay	IC50=3.83673 μM	SANGER
BC-1	Growth Inhibition Assay	IC50=3.7402 μM	SANGER
MZ7-mel	Growth Inhibition Assay	IC50=3.66099 μM	SANGER
MRK-nu-1	Growth Inhibition Assay	IC50=3.61468 μM	SANGER
MZ1-PC	Growth Inhibition Assay	IC50=3.47509 μM	SANGER
TE-5	Growth Inhibition Assay	IC50=3.13162 μM	SANGER
HCC2218	Growth Inhibition Assay	IC50=3.12003 μM	SANGER
HL-60	Growth Inhibition Assay	IC50=3.06299 μM	SANGER
MFH-ino	Growth Inhibition Assay	IC50=2.92185 μM	SANGER
KMOE-2	Growth Inhibition Assay	IC50=2.8135 μM	SANGER
L-540	Growth Inhibition Assay	IC50=2.75789 μM	SANGER
K052	Growth Inhibition Assay	IC50=2.74616 μM	SANGER
BE-13	Growth Inhibition Assay	IC50=2.69609 μM	SANGER
SIG-M5	Growth Inhibition Assay	IC50=2.42242 μM	SANGER
NCI-H2171	Growth Inhibition Assay	IC50=2.39764 μM	SANGER
NCI-SNU-1	Growth Inhibition Assay	IC50=2.3162 μM	SANGER
OVCAR-4	Growth Inhibition Assay	IC50=2.21393 μM	SANGER
D-247MG	Growth Inhibition Assay	IC50=2.1448 μM	SANGER
A3-KAW	Growth Inhibition Assay	IC50=1.8842 μM	SANGER
MEG-01	Growth Inhibition Assay	IC50=1.8098 μM	SANGER
SF126	Growth Inhibition Assay	IC50=1.63812 μM	SANGER
no-10	Growth Inhibition Assay	IC50=1.61726 μM	SANGER
A388	Growth Inhibition Assay	IC50=1.59165 μM	SANGER
KG-1	Growth Inhibition Assay	IC50=1.47935 μM	SANGER
LAMA-84	Growth Inhibition Assay	IC50=1.37648 μM	SANGER
EM-2	Growth Inhibition Assay	IC50=1.35578 μM	SANGER
NCI-H1436	Growth Inhibition Assay	IC50=1.21678 μM	SANGER
LB2518-MEL	Growth Inhibition Assay	IC50=1.20809 μM	SANGER
KM12	Growth Inhibition Assay	IC50=1.02098 μM	SANGER
GDM-1	Growth Inhibition Assay	IC50=0.90698 μM	SANGER
HCC2998	Growth Inhibition Assay	IC50=0.88818 μM	SANGER
HOP-62	Growth Inhibition Assay	IC50=0.85088 μM	SANGER
SH-4	Growth Inhibition Assay	IC50=0.65613 μM	SANGER
NOS-1	Growth Inhibition Assay	IC50=0.5636 μM	SANGER
BB65-RCC	Growth Inhibition Assay	IC50=0.47073 μM	SANGER
CGTH-W-1	Growth Inhibition Assay	IC50=0.25022 μM	SANGER
NKM-1	Growth Inhibition Assay	IC50=0.07416 μM	SANGER
ALL-PO	Growth Inhibition Assay	IC50=0.03184 μM	SANGER
MONO-MAC-6	Growth Inhibition Assay	IC50=0.00418 μM	SANGER
MV-4-11	Growth Inhibition Assay	IC50=0.00000303 μM	SANGER
NCI-SNU-16	Growth Inhibition Assay	IC50=9.21026 μM	SANGER
SHP-77	Growth Inhibition Assay	IC50=9.71662 μM	SANGER
A4-Fuk	Growth Inhibition Assay	IC50=9.7561 μM	SANGER
NB6	Growth Inhibition Assay	IC50=9.76029 μM	SANGER
JiyoyeP-2003	Growth Inhibition Assay	IC50=10.4745 μM	SANGER
DMS-114	Growth Inhibition Assay	IC50=10.5441 μM	SANGER
NB7	Growth Inhibition Assay	IC50=10.7526 μM	SANGER
NCI-H747	Growth Inhibition Assay	IC50=11.1216 μM	SANGER
HH	Growth Inhibition Assay	IC50=11.3876 μM	SANGER
EW-18	Growth Inhibition Assay	IC50=11.9044 μM	SANGER
CHP-126	Growth Inhibition Assay	IC50=11.9738 μM	SANGER
NTERA-S-cl-D1	Growth Inhibition Assay	IC50=12.0278 μM	SANGER
DEL	Growth Inhibition Assay	IC50=12.0985 μM	SANGER
LU-139	Growth Inhibition Assay	IC50=12.5413 μM	SANGER
P30-OHK	Growth Inhibition Assay	IC50=12.5479 μM	SANGER
NCI-H1522	Growth Inhibition Assay	IC50=12.746 μM	SANGER
NCI-H1299	Growth Inhibition Assay	IC50=13.2911 μM	SANGER
UACC-257	Growth Inhibition Assay	IC50=13.5126 μM	SANGER
Calu-6	Growth Inhibition Assay	IC50=13.6046 μM	SANGER
NCI-H1882	Growth Inhibition Assay	IC50=13.8555 μM	SANGER
BB30-HNC	Growth Inhibition Assay	IC50=14.0609 μM	SANGER
ES1	Growth Inhibition Assay	IC50=14.1551 μM	SANGER
NCI-H1694	Growth Inhibition Assay	IC50=14.4811 μM	SANGER
IST-SL1	Growth Inhibition Assay	IC50=14.9616 μM	SANGER
ECC4	Growth Inhibition Assay	IC50=15.0558 μM	SANGER
MDA-MB-134-VI	Growth Inhibition Assay	IC50=15.4131 μM	SANGER
SCH	Growth Inhibition Assay	IC50=15.4728 μM	SANGER
SK-N-FI	Growth Inhibition Assay	IC50=15.6534 μM	SANGER
HDLM-2	Growth Inhibition Assay	IC50=16.0714 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay	IC50=16.1297 μM	SANGER
EW-24	Growth Inhibition Assay	IC50=16.1661 μM	SANGER
NCI-H2141	Growth Inhibition Assay	IC50=16.189 μM	SANGER
LC4-1	Growth Inhibition Assay	IC50=16.6119 μM	SANGER
HT-144	Growth Inhibition Assay	IC50=17.006 μM	SANGER
SK-MEL-1	Growth Inhibition Assay	IC50=17.0072 μM	SANGER
SCC-15	Growth Inhibition Assay	IC50=17.1638 μM	SANGER
C8166	Growth Inhibition Assay	IC50=17.6833 μM	SANGER
GOTO	Growth Inhibition Assay	IC50=17.8344 μM	SANGER
COR-L279	Growth Inhibition Assay	IC50=18.1362 μM	SANGER
K-562	Growth Inhibition Assay	IC50=18.7143 μM	SANGER
ES3	Growth Inhibition Assay	IC50=18.8041 μM	SANGER
LU-165	Growth Inhibition Assay	IC50=19.7008 μM	SANGER
KM-H2	Growth Inhibition Assay	IC50=20.3184 μM	SANGER
RL	Growth Inhibition Assay	IC50=20.9692 μM	SANGER
EW-3	Growth Inhibition Assay	IC50=21.1889 μM	SANGER
A101D	Growth Inhibition Assay	IC50=21.3752 μM	SANGER
HUTU-80	Growth Inhibition Assay	IC50=21.3946 μM	SANGER
NCI-H23	Growth Inhibition Assay	IC50=21.3992 μM	SANGER
PF-382	Growth Inhibition Assay	IC50=21.4403 μM	SANGER
LB373-MEL-D	Growth Inhibition Assay	IC50=21.5615 μM	SANGER
TE-8	Growth Inhibition Assay	IC50=21.6394 μM	SANGER
TE-9	Growth Inhibition Assay	IC50=21.8513 μM	SANGER
Daudi	Growth Inhibition Assay	IC50=21.9304 μM	SANGER
D-542MG	Growth Inhibition Assay	IC50=22.0256 μM	SANGER
U-698-M	Growth Inhibition Assay	IC50=22.4603 μM	SANGER
ES6	Growth Inhibition Assay	IC50=22.7366 μM	SANGER
DU-4475	Growth Inhibition Assay	IC50=23.8897 μM	SANGER
ECC12	Growth Inhibition Assay	IC50=24.2803 μM	SANGER
C2BBe1	Growth Inhibition Assay	IC50=24.3239 μM	SANGER
IST-SL2	Growth Inhibition Assay	IC50=24.4362 μM	SANGER
DJM-1	Growth Inhibition Assay	IC50=24.5221 μM	SANGER
DMS-153	Growth Inhibition Assay	IC50=24.8614 μM	SANGER
NB13	Growth Inhibition Assay	IC50=25.0265 μM	SANGER
SK-N-DZ	Growth Inhibition Assay	IC50=26.3414 μM	SANGER
COR-L88	Growth Inhibition Assay	IC50=26.5796 μM	SANGER
LU-65	Growth Inhibition Assay	IC50=26.8535 μM	SANGER
TGBC1TKB	Growth Inhibition Assay	IC50=26.9828 μM	SANGER
THP-1	Growth Inhibition Assay	IC50=27.2141 μM	SANGER
ONS-76	Growth Inhibition Assay	IC50=27.332 μM	SANGER
LC-2-ad	Growth Inhibition Assay	IC50=27.6231 μM	SANGER
EW-13	Growth Inhibition Assay	IC50=29.1746 μM	SANGER
MS-1	Growth Inhibition Assay	IC50=30.7278 μM	SANGER
NCI-H2227	Growth Inhibition Assay	IC50=30.9806 μM	SANGER
LXF-289	Growth Inhibition Assay	IC50=31.4492 μM	SANGER
MC116	Growth Inhibition Assay	IC50=32.0826 μM	SANGER
EVSA-T	Growth Inhibition Assay	IC50=32.2585 μM	SANGER
CTB-1	Growth Inhibition Assay	IC50=33.1101 μM	SANGER
COLO-320-HSR	Growth Inhibition Assay	IC50=33.1603 μM	SANGER
NCI-H2196	Growth Inhibition Assay	IC50=33.2557 μM	SANGER
LB2241-RCC	Growth Inhibition Assay	IC50=33.3135 μM	SANGER
LS-513	Growth Inhibition Assay	IC50=33.8638 μM	SANGER
LP-1	Growth Inhibition Assay	IC50=33.9956 μM	SANGER
A253	Growth Inhibition Assay	IC50=34.2296 μM	SANGER
SK-MM-2	Growth Inhibition Assay	IC50=34.9451 μM	SANGER
NCI-H1963	Growth Inhibition Assay	IC50=35.3072 μM	SANGER
MMAC-SF	Growth Inhibition Assay	IC50=35.8785 μM	SANGER
LB831-BLC	Growth Inhibition Assay	IC50=36.0654 μM	SANGER
WSU-NHL	Growth Inhibition Assay	IC50=36.164 μM	SANGER
CESS	Growth Inhibition Assay	IC50=36.2848 μM	SANGER
NEC8	Growth Inhibition Assay	IC50=36.5835 μM	SANGER
KNS-42	Growth Inhibition Assay	IC50=37.1237 μM	SANGER
MHH-CALL-2	Growth Inhibition Assay	IC50=37.1821 μM	SANGER
K5	Growth Inhibition Assay	IC50=38.43 μM	SANGER
CP66-MEL	Growth Inhibition Assay	IC50=39.0733 μM	SANGER
OPM-2	Growth Inhibition Assay	IC50=39.8432 μM	SANGER
IST-MES1	Growth Inhibition Assay	IC50=40.3096 μM	SANGER
EC-GI-10	Growth Inhibition Assay	IC50=41.5805 μM	SANGER
CTV-1	Growth Inhibition Assay	IC50=42.8406 μM	SANGER
DG-75	Growth Inhibition Assay	IC50=43.7595 μM	SANGER
KNS-81-FD	Growth Inhibition Assay	IC50=45.4058 μM	SANGER
NCI-H82	Growth Inhibition Assay	IC50=45.5758 μM	SANGER
RPMI-8866	Growth Inhibition Assay	IC50=46.1873 μM	SANGER
ACN	Growth Inhibition Assay	IC50=46.434 μM	SANGER
NCI-H1395	Growth Inhibition Assay	IC50=46.4756 μM	SANGER
NCI-H209	Growth Inhibition Assay	IC50=47.1405 μM	SANGER
TGW	Growth Inhibition Assay	IC50=49.0791 μM	SANGER
NCI-H748	Growth Inhibition Assay	IC50=49.4753 μM	SANGER
EKVX	Growth Inhibition Assay	IC50=49.6628 μM	SANGER
MV4-11	Antiproliferative activity assay	IC50 = 0.00087 μM	19754199
MV4-11	Cytotoxicity assay	IC50 = 0.00087 μM	19654408
TT	Antiproliferative activity assay	IC50 = 0.0014 μM	18849971
RS4-11	Function assay	IC50 = 0.002 μM	19654408
MOLM13	Function assay	IC50 = 0.002 μM	24641103
Sf9	Function assay	IC50 = 0.003 μM	21708468
RS4-11	Function assay	IC50 = 0.0032 μM	19654408
MV4-11	Growth inhibition assay	IC50 = 0.004 μM	29357250
A375	Function assay	IC50 = 0.0044 μM	29461827
MOLM13	Antiproliferative activity assay	IC50 = 0.005 μM	24641103
MV4-11	Function assay	IC50 = 0.007 μM	23362959
MV4-11	Cytotoxicity assay	IC50 = 0.007 μM	26342867
HEK293	Function assay	Kd = 0.013 μM	19754199
Kasumi-1	Antiproliferative activity assay	IC50 = 0.015 μM	20570526
MV4-11	Antiproliferative activity assay	IC50 = 0.015 μM	20570526
sf9	Function assay	IC50 = 0.015 μM	29266937
sf9	Function assay	IC50 = 0.018 μM	21708468
sf9	Function assay	IC50 = 0.02 μM	23618709
MV4-11	Antiproliferative activity assay	GI50 = 0.03 μM	21708468
Sf9	Function assay	IC50 = 0.042 μM	26081023
SF9	Function assay	IC50 = 0.043 μM	18473434
MV4-11	Cytotoxicity assay	GI50 = 0.043 μM	23618709
MV4-11	Function assay	GI50 = 0.043 μM	26081023
SF9	Function assay	IC50 = 0.044 μM	26081023
SF9	Function assay	IC50 = 0.054 μM	21708468
SF9	Function assay	IC50 = 0.054 μM	23618709
MOLM13	Antiproliferative activity assay	GI50 = 0.056 μM	21708468
MOLM13	Antiproliferative activity assay	GI50 = 0.056 μM	22726931
MOLM13	Cytotoxicity assay	GI50 = 0.056 μM	23618709
MOLM-13	Function assay	GI50 = 0.056 μM	26081023
SF9	Function assay	IC50 = 0.058 μM	29266937
WM266.4	Antiproliferative activity assay	IC50 = 0.06 μM	25496804
MDA-MB-231	Function assay	IC50 = 0.063 μM	28431342
SF9	Function assay	IC50 = 0.09 μM	29266937
Spodoptera frugiperda	Function assay	IC50 = 0.09 μM	26922228
SF9	Function assay	IC50 = 0.09 μM	23562241
SF9	Function assay	IC50 = 0.1 μM	23442188
SF9	Function assay	IC50 = 0.1 μM	23442188
HEK293	Function assay	IC50 = 0.12 μM	26318998
MCF7	Antiproliferative activity assay	IC50 = 0.19 μM	25496804
MV4-11	Antiproliferative activity human	IC50 = 0.3 μM	28242553
HepG2	Antiproliferative activity assay	EC50 = 0.302 μM	27010810
THP1	Antiproliferative activity assay	IC50 = 0.31 μM	20570526
SMMC7721	Cytotoxicity assay	IC50 = 0.37 μM	25982075
HT-29	Antiproliferative activity assay	IC50 = 0.39 μM	25778995
sf9	Function assay	Kd = 0.6 μM	28109791
T47D	Antiproliferative activity assay	IC50 = 0.61 μM	25778995
A549	Cytotoxicity assay	IC50 = 0.63 μM	25982075
HeLa	Cytotoxicity assay	IC50 = 0.64 μM	30015070
WM3629	Antiproliferative activity assay	GI50 = 0.65 μM	20466542
SMMC7721	Antiproliferative activity assay	IC50 = 0.65 μM	26342134
WM3629	Growth inhibition assay	GI50 = 0.78 μM	20149658
WM3629	Antiproliferative activity assay	GI50 = 0.78 μM	26810260
MCF7	Antiproliferative activity assay	IC50 = 0.78 μM	25778995
K562	Antiproliferative activity assay	IC50 = 0.86 μM	24315192
COLO205	Antiproliferative activity assay	IC50 = 0.87 μM	25778995
T29	Cytotoxicity assay	IC50 = 0.9 μM	26318998
MDA-MB-231	Cytotoxicity assay	IC50 = 0.94 μM	25086238
MDA-MB-231	Cytotoxicity assay	IC50 = 0.94 μM	25440879
HepG2	Antiproliferative activity assay	IC50 = 1.06 μM	29628325
BL21(DE3)	Function assay	IC50 = 1.1 μM	19928858
K562	Antiproliferative activity assay	IC50 = 1.22 μM	25778995
MDA-MB-231	Growth inhibition assay	GI50 = 1.26 μM	28088086
MDA-MB-231	Cytotoxicity assay	GI50 = 1.26 μM	26590508
MDA-MB-231	Antiproliferative activity assay	GI50 = 1.26 μM	27017549
SK-MEL-28	Antiproliferative activity assay	EC50 = 1.3 μM	18942827
sf9	Function assay	Kd = 1.3 μM	28109791
F-6-8	Cytotoxicity assay	IC50 = 1.3 μM	26318998
A549	Antiproliferative activity assay	IC50 = 1.45 μM	26342134
rhabdomyosarcoma	Antiviral activity assay	EC50 = 1.5 μM	27288186
HL-60(TB)	Growth inhibition assay	GI50 = 1.58 μM	28088086
RPMI8226	Growth inhibition assay	GI50 = 1.58 μM	28088086
KM12	Growth inhibition assay	GI50 = 1.58 μM	28088086
LOXIMVI	Growth inhibition assay	GI50 = 1.58 μM	28088086
HCT116	Growth inhibition assay	GI50 = 1.58 μM	28088086
HOP92	Growth inhibition assay	GI50 = 1.58 μM	28088086
SF539	Growth inhibition assay	GI50 = 1.58 μM	28088086
UACC62	Growth inhibition assay	GI50 = 1.58 μM	28088086
SF295	Growth inhibition assay	GI50 = 1.58 μM	28088086
MDA-MB-435	Growth inhibition assay	GI50 = 1.58 μM	28088086
SK-MEL-5	Growth inhibition assay	GI50 = 1.58 μM	28088086
T47D	Growth inhibition assay	GI50 = 1.58 μM	28088086
RPMI8266	Cytotoxicity assay	GI50 = 1.58 μM	26590508
HL-60(TB)	Cytotoxicity assay	GI50 = 1.58 μM	26590508
KM12	Cytotoxicity assay	GI50 = 1.58 μM	26590508
HCT116	Cytotoxicity assay	GI50 = 1.58 μM	26590508
SF295	Cytotoxicity assay	GI50 = 1.58 μM	26590508
SF539	Cytotoxicity assay	GI50 = 1.58 μM	26590508
SK-MEL-2	Cytotoxicity assay	GI50 = 1.58 μM	26590508
MDA-MB-435	Cytotoxicity assay	GI50 = 1.58 μM	26590508
SK-MEL-5	Cytotoxicity assay	GI50 = 1.58 μM	26590508
LOXIMVI	Cytotoxicity assay	GI50 = 1.58 μM	26590508
T47D	Cytotoxicity assay	GI50 = 1.58 μM	26590508
SMMC7721	Antiproliferative activity assay	IC50 = 1.58 μM	26753815
LOXIMVI	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
UACC62	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
SK-MEL-5	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
KM12	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
MDA-MB-435	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
SF539	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
SF295	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
HCT116	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
HOP92	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
RPMI8226	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
HL-60(TB)	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
T47D	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
7dF3	Function assay	IC50 = 1.62 μM	29266937
MDA-MB-435	Antiproliferative activity assay	IC50 = 1.67 μM	25778995
HL60	Cytotoxicity assay	IC50 = 1.68 μM	24858546
SW579	Antiproliferative activity human	IC50 = 1.73 μM	28242553
MCF7	Antiproliferative activity assay	IC50 = 1.88 μM	25637123
A375P	Antiproliferative activity assay	IC50 = 1.9 μM	24128410
A549	Cytotoxicity assay	IC50 = 1.92 μM	24826815
HCT116	Antiproliferative activity assay	IC50 = 2 μM	22808911
MDA-MB-231	Cytotoxicity assay	IC50 = 2 μM	23454017
NCI-H23	Growth inhibition assay	GI50 = 2 μM	28088086
NCI-H522	Growth inhibition assay	GI50 = 2 μM	28088086
HOP62	Growth inhibition assay	GI50 = 2 μM	28088086
NCI-H226	Growth inhibition assay	GI50 = 2 μM	28088086
HT-29	Growth inhibition assay	GI50 = 2 μM	28088086
U251	Growth inhibition assay	GI50 = 2 μM	28088086
COLO205	Growth inhibition assay	GI50 = 2 μM	28088086
CCRF-CEM	Growth inhibition assay	GI50 = 2 μM	28088086
MALME-3M	Growth inhibition assay	GI50 = 2 μM	28088086
M14	Growth inhibition assay	GI50 = 2 μM	28088086
UACC257	Growth inhibition assay	GI50 = 2 μM	28088086
PC3	Growth inhibition assay	GI50 = 2 μM	28088086
SK-MEL-2	Growth inhibition assay	GI50 = 2 μM	28088086
MDA-MB-468	Growth inhibition assay	GI50 = 2 μM	28088086
CCRF-CEM	Cytotoxicity assay	GI50 = 2 μM	26590508
NCI-H23	Cytotoxicity assay	GI50 = 2 μM	26590508
NCI-H522	Cytotoxicity assay	GI50 = 2 μM	26590508
COLO205	Cytotoxicity assay	GI50 = 2 μM	26590508
HT-29	Cytotoxicity assay	GI50 = 2 μM	26590508
SK-MEL-28	Cytotoxicity assay	GI50 = 2 μM	26590508
HOP62	Cytotoxicity assay	GI50 = 2 μM	26590508
UACC257	Cytotoxicity assay	GI50 = 2 μM	26590508
NCI-H226	Cytotoxicity assay	GI50 = 2 μM	26590508
U251	Cytotoxicity assay	GI50 = 2 μM	26590508
PC3	Cytotoxicity assay	GI50 = 2 μM	26590508
M14	Cytotoxicity assay	GI50 = 2 μM	26590508
MDA-MB-468	Cytotoxicity assay	GI50 = 2 μM	26590508
PC3	Antiproliferative activity assay	GI50 = 2 μM	27017549
MALME-3M	Antiproliferative activity assay	GI50 = 2 μM	27017549
U251	Antiproliferative activity assay	GI50 = 2 μM	27017549
UACC257	Antiproliferative activity assay	GI50 = 2 μM	27017549
SK-MEL-2	Antiproliferative activity assay	GI50 = 2 μM	27017549
COLO205	Antiproliferative activity assay	GI50 = 2 μM	27017549
NCI-H23	Antiproliferative activity assay	GI50 = 2 μM	27017549
HT-29	Antiproliferative activity assay	GI50 = 2 μM	27017549
M14	Antiproliferative activity assay	GI50 = 2 μM	27017549
NCI-H226	Antiproliferative activity assay	GI50 = 2 μM	27017549
HOP62	Antiproliferative activity assay	GI50 = 2 μM	27017549
MDA-MB-468	Antiproliferative activity assay	GI50 = 2 μM	27017549
CCRF-CEM	Antiproliferative activity assay	GI50 = 2 μM	27017549
NCI-H522	Antiproliferative activity assay	GI50 = 2 μM	27017549
A549	Antiproliferative activity assay	IC50 = 2.02 μM	26753815
MDA-MB-435	Growth inhibition assay	IC50 = 2.11 μM	29189002
NCI-H460	Antiproliferative activity assay	IC50 = 2.19 μM	30216849
H460	Cytotoxicity assay	IC50 = 2.19 μM	24826815
H460	Cytotoxicity assay	IC50 = 2.19 μM	25086238
H460	Cytotoxicity assay	IC50 = 2.19 μM	25440879
A375	Toxicity assay	IC50 = 2.2 μM	19654408
H460	Antiproliferative activity assay	IC50 = 2.25 μM	26991938
HCT116	Antiproliferative activity assay	IC50 = 2.3 μM	23260578
MKN45	Antiproliferative activity assay	IC50 = 2.32 μM	30216849
MKN45	Cytotoxicity assay	IC50 = 2.32 μM	24826815
MKN45	Cytotoxicity assay	IC50 = 2.32 μM	25086238
MKN45	Cytotoxicity assay	IC50 = 2.32 μM	25440879
U937	Antiproliferative activity assay	GI50 = 2.34 μM	29459144
A375	Antiproliferative activity assay	IC50 = 2.4 μM	22808911
HeLa	Growth inhibition assay	IC50 = 2.44 μM	29102175
MDA-MB-231	Cytotoxicity assay	IC50 = 2.5 μM	22414612
MCF7	Antiproliferative activity assay	IC50 = 2.51 μM	30216849
UO31	Antiproliferative activity assay	IC50 = 2.51 μM	30216849
NCI-H322M	Growth inhibition assay	GI50 = 2.51 μM	28088086
NCI-H460	Growth inhibition assay	GI50 = 2.51 μM	28088086
KM12	Growth inhibition assay	TGI = 2.51 μM	28088086
LOXIMVI	Growth inhibition assay	TGI = 2.51 μM	28088086
EKVX	Growth inhibition assay	GI50 = 2.51 μM	28088086
HCT116	Growth inhibition assay	TGI = 2.51 μM	28088086
SW620	Growth inhibition assay	GI50 = 2.51 μM	28088086
SF268	Growth inhibition assay	GI50 = 2.51 μM	28088086
SF539	Growth inhibition assay	TGI = 2.51 μM	28088086
A498	Growth inhibition assay	GI50 = 2.51 μM	28088086
UACC62	Growth inhibition assay	TGI = 2.51 μM	28088086
IGROV1	Growth inhibition assay	GI50 = 2.51 μM	28088086
HCT15	Growth inhibition assay	GI50 = 2.51 μM	28088086
SK-MEL-28	Growth inhibition assay	GI50 = 2.51 μM	28088086
SK-MEL-28	Growth inhibition assay	TGI = 2.51 μM	28088086
ACHN	Growth inhibition assay	GI50 = 2.51 μM	28088086
SK-MEL-5	Growth inhibition assay	TGI = 2.51 μM	28088086
NCI/ADR-RES	Growth inhibition assay	GI50 = 2.51 μM	28088086
MCF7	Growth inhibition assay	GI50 = 2.51 μM	28088086
SN12C	Growth inhibition assay	GI50 = 2.51 μM	28088086
Hs 578T	Growth inhibition assay	GI50 = 2.51 μM	28088086
SKOV3	Growth inhibition assay	GI50 = 2.51 μM	28088086
UO31	Growth inhibition assay	GI50 = 2.51 μM	28088086
NCI-H460	Cytotoxicity assay	GI50 = 2.51 μM	26590508
HCT15	Cytotoxicity assay	GI50 = 2.51 μM	26590508
SW620	Cytotoxicity assay	GI50 = 2.51 μM	26590508
SF268	Cytotoxicity assay	GI50 = 2.51 μM	26590508
IGROV1	Cytotoxicity assay	GI50 = 2.51 μM	26590508
OVCAR8	Cytotoxicity assay	GI50 = 2.51 μM	26590508
NCI/ADR-RES	Cytotoxicity assay	GI50 = 2.51 μM	26590508
SKOV3	Cytotoxicity assay	GI50 = 2.51 μM	26590508
SN12C	Cytotoxicity assay	GI50 = 2.51 μM	26590508
NCI-H322M	Cytotoxicity assay	GI50 = 2.51 μM	26590508
MCF7	Cytotoxicity assay	GI50 = 2.51 μM	26590508
UO31	Cytotoxicity assay	GI50 = 2.51 μM	26590508
Hs578T	Cytotoxicity assay	GI50 = 2.51 μM	26590508
A498	Cytotoxicity assay	GI50 = 2.51 μM	26590508
A498	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
SKOV3	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
UO31	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
NCI-ADR-RES	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
SN12C	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
IGROV1	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
ACHN	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
OVCAR8	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
SK-MEL-28	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
NCI-H322M	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
SF268	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
HCT15	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
NCI-H460	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
SW620	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
EKVX	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
MCF7	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
Hs 578T	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
HT-29	Antiproliferative activity assay	IC50 = 2.58 μM	29886324
A375P	Antiproliferative activity assay	GI50 = 2.58 μM	26810260
TPC1	Antiproliferative activity assay	EC50 = 2.6 μM	22559926
Hep3B	Growth inhibition assay	IC50 = 2.63 μM	29102175
A375P	Antiproliferative activity assay	IC50 = 2.7 μM	22460030
U937	Antiproliferative activity assay	GI50 = 2.74 μM	26318067
U937	Cytotoxicity assay	GI50 = 2.74 μM	24878193
MCF7	Growth inhibition assay	IC50 = 2.78 μM	29102175
MDA-MB-231	Antiproliferative activity assay	IC50 = 2.8 μM	29202403
HepG2	Antiproliferative activity assay	IC50 = 2.84 μM	28242553
U937	Growth inhibition assay	GI50 = 2.85 μM	22014755
A549	Cytotoxicity assay	IC50 = 2.92 μM	28927801
A549	Cytotoxicity assay	IC50 = 2.92 μM	27777009
ZR75-30	Growth inhibition assay	IC50 = 2.96 μM	29102175
PC3	Cytotoxicity assay	IC50 = 3.03 μM	28340913
MDA-MB-231	Antiproliferative activity assay	IC50 = 3.08 μM	26991938
A549	Growth inhibition assay	IC50 = 3.1 μM	29102175
K562	Growth inhibition assay	GI50 = 3.16 μM	28088086
MOLT4	Growth inhibition assay	GI50 = 3.16 μM	28088086
A549/ATCC	Growth inhibition assay	GI50 = 3.16 μM	28088086
RPMI8226	Growth inhibition assay	TGI = 3.16 μM	28088086
SR	Growth inhibition assay	GI50 = 3.16 μM	28088086
HOP62	Growth inhibition assay	TGI = 3.16 μM	28088086
NCI-H226	Growth inhibition assay	TGI = 3.16 μM	28088086
U251	Growth inhibition assay	TGI = 3.16 μM	28088086
COLO205	Growth inhibition assay	TGI = 3.16 μM	28088086
M14	Growth inhibition assay	TGI = 3.16 μM	28088086
HCC2998	Growth inhibition assay	GI50 = 3.16 μM	28088086
SNB75	Growth inhibition assay	GI50 = 3.16 μM	28088086
786-0	Growth inhibition assay	GI50 = 3.16 μM	28088086
A498	Growth inhibition assay	TGI = 3.16 μM	28088086
HCT15	Growth inhibition assay	TGI = 3.16 μM	28088086
OVCAR3	Growth inhibition assay	GI50 = 3.16 μM	28088086
OVCAR4	Growth inhibition assay	GI50 = 3.16 μM	28088086
Caki1	Growth inhibition assay	GI50 = 3.16 μM	28088086
SNB19	Growth inhibition assay	GI50 = 3.16 μM	28088086
OVCAR5	Growth inhibition assay	GI50 = 3.16 μM	28088086
DU145	Growth inhibition assay	GI50 = 3.16 μM	28088086
OVCAR8	Growth inhibition assay	GI50 = 3.16 μM	28088086
SN12C	Growth inhibition assay	TGI = 3.16 μM	28088086
MDA-MB-231	Growth inhibition assay	TGI = 3.16 μM	28088086
RXF393	Growth inhibition assay	GI50 = 3.16 μM	28088086
BT549	Growth inhibition assay	GI50 = 3.16 μM	28088086
K562	Cytotoxicity assay	GI50 = 3.16 μM	26590508
MOLT4	Cytotoxicity assay	GI50 = 3.16 μM	26590508
SNB19	Cytotoxicity assay	GI50 = 3.16 μM	26590508
SR	Cytotoxicity assay	GI50 = 3.16 μM	26590508
A549	Cytotoxicity assay	GI50 = 3.16 μM	26590508
OVCAR3	Cytotoxicity assay	GI50 = 3.16 μM	26590508
OVCAR4	Cytotoxicity assay	GI50 = 3.16 μM	26590508
SNB75	Cytotoxicity assay	GI50 = 3.16 μM	26590508
OVCAR5	Cytotoxicity assay	GI50 = 3.16 μM	26590508
DU145	Cytotoxicity assay	GI50 = 3.16 μM	26590508
786-0	Cytotoxicity assay	GI50 = 3.16 μM	26590508
BT549	Cytotoxicity assay	GI50 = 3.16 μM	26590508
ACHN	Cytotoxicity assay	GI50 = 3.16 μM	26590508
Caki1	Cytotoxicity assay	GI50 = 3.16 μM	26590508
786-0	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
LOXIMVI	Antiproliferative activity assay	TGI = 3.16 μM	27017549
Caki1	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
OVCAR5	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
RXF393	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
SNB75	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
OVCAR3	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
SNB19	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
SK-MEL-5	Antiproliferative activity assay	TGI = 3.16 μM	27017549
OVCAR4	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
SK-MEL-2	Antiproliferative activity assay	TGI = 3.16 μM	27017549
BT549	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
MOLT4	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
K562	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
HCC2998	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
HCC2998	Antiproliferative activity assay	TGI = 3.16 μM	27017549
A549/ATCC	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
DU145	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
SR	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
MCF7	Cytotoxicity assay	IC50 = 3.18 μM	28927801
PC3	Cytotoxicity assay	IC50 = 3.18 μM	28927801
MCF7	Cytotoxicity assay	IC50 = 3.18 μM	27777009
A549	Antiproliferative activity assay	IC50 = 3.19 μM	25778995
PC3	Cytotoxicity assay	IC50 = 3.24 μM	27777009
HeLa	Function assay	IC50 = 3.3 μM	15225706
HeLa	Function assay	IC50 = 3.3 μM	15225706
LoVo	Cytotoxicity assay	IC50 = 3.3 μM	23454017
A375	Antiproliferative activity assay	IC50 = 3.36 μM	29602674
HT-29	Antiproliferative activity assay	IC50 = 3.37 μM	26991938
FLT3 gene-deficient U937	Antiproliferative activity assay	GI50 = 3.4 μM	21708468
FLT3 negative U937	Cytotoxicity assay	GI50 = 3.4 μM	23618709
U937	Cytotoxicity assay	GI50 = 3.4 μM	26081023
A375P	Antiproliferative activity assay	GI50 = 3.4 μM	29459144
ACHN	Cytotoxicity assay	IC50 = 3.4 μM	29517908
ACHN	Cytotoxicity assay	IC50 = 3.4 μM	29297688
HepG2	Function assay	IC50 = 3.4 μM	26071861
A375P	Cytotoxicity assay	GI50 = 3.4 μM	24878193
HepG2	Cytotoxicity assay	IC50 = 3.44 μM	28927801
HepG2	Cytotoxicity assay	IC50 = 3.44 μM	27777009
ACHN	Cytotoxicity assay	IC50 = 3.5 μM	29786436
HepG2	Antiproliferative activity assay	IC50 = 3.5 μM	25462265
HT-29	Cytotoxicity assay	IC50 = 3.61 μM	24826815
HT-29	Antiproliferative activity assay	IC50 = 3.61 μM	30216849
HT-29	Cytotoxicity assay	IC50 = 3.61 μM	25086238
HT-29	Cytotoxicity assay	IC50 = 3.61 μM	25440879
MCF7	Anticancer activity assay	IC50 = 3.64 μM	29549841
Sf9	Function assay	IC50 = 3.8 μM	21708468
Sf9	Function assay	IC50 = 3.8 μM	23618709
Sf9	Function assay	IC50 = 3.8 μM	26081023
A2058	Cytotoxicity assay	IC50 = 3.8 μM	22708987
NCI-H460	Cytotoxicity assay	IC50 = 3.9 μM	23454017
SK-MEL-30	Cytotoxicity assay	IC50 = 3.9 μM	29461827
HT-29	Anticancer activity assay	IC50 = 3.97 μM	29549841
SF268	Growth inhibition assay	TGI = 3.98 μM	28088086
SNB75	Growth inhibition assay	TGI = 3.98 μM	28088086
OVCAR3	Growth inhibition assay	TGI = 3.98 μM	28088086
SNB19	Growth inhibition assay	TGI = 3.98 μM	28088086
Hs 578T	Growth inhibition assay	TGI = 3.98 μM	28088086
TK10	Growth inhibition assay	GI50 = 3.98 μM	28088086
BT549	Growth inhibition assay	TGI = 3.98 μM	28088086
Caki1	Antiproliferative activity assay	TGI = 3.98 μM	27017549
TK10	Antiproliferative activity assay	GI50 = 3.98 μM	27017549
MDA-MB-435	Antiproliferative activity assay	TGI = 3.98 μM	27017549
HCT116	Antiproliferative activity assay	TGI = 3.98 μM	27017549
MDA-MB-231	Antiproliferative activity assay	TGI = 3.98 μM	27017549
HepG2	Cytotoxicity assay	IC50 = 4 μM	23454017
HT-29	Cytotoxicity assay	IC50 = 4 μM	23454017
A549	Cytotoxicity assay	IC50 = 4 μM	23454017
HuH7	Cytotoxicity assay	GI50 = 4 μM	23726028
PC3	Antiproliferative activity assay	IC50 = 4.13 μM	25778995
HeLa	Cytotoxicity assay	IC50 = 4.163 μM	23362959
MDA-MB-436	Antiproliferative activity assay	IC50 = 4.2 μM	29202403
MCF7	Cytotoxicity assay	IC50 = 4.21 μM	27043268
MCF7	Cytotoxicity assay	IC50 = 4.21 μM	28340913
LOXIMVI	Antiproliferative activity assay	IC50 = 4.25 μM	25778995
OVCAR4	Cytotoxicity assay	TGI = 4.31 μM	26590508
WM1361	Antiproliferative activity assay	GI50 = 4.345 μM	20148563
WM266.4	Growth inhibition assay	GI50 = 4.5 μM	20199087
HepG2	Cytotoxicity assay	GI50 = 4.5 μM	23726028
A549	Antiproliferative activity assay	IC50 = 4.5 μM	23260578
LS174T	Function assay	IC50 = 4.52 μM	29266937
8505C	Antiproliferative activity assay	IC50 = 4.7 μM	29032031
OVCAR8	Cytotoxicity assay	TGI = 4.73 μM	26590508
MDA-MB-231	Cytotoxicity assay	IC50 = 4.77 μM	20435479
B16-F1	Antiproliferative activity assay	IC50 = 4.9 μM	18477505
WM164	Antiproliferative activity assay	IC50 = 4.9 μM	17561392
B16-F1	Antiproliferative activity assay	IC50 = 4.9 μM	20056548
MDA-MB-468	Cytotoxicity assay	IC50 = 4.9 μM	26159483
786-O	Cytotoxicity assay	IC50 = 4.9 μM	29517908
786-O	Cytotoxicity assay	IC50 = 4.9 μM	29297688
WM266.4	Antiproliferative activity assay	GI50 = 4.933 μM	20148563
WM266.4	Growth inhibition assay	IC50 = 5 μM	19323560
WM164	Antiproliferative activity assay	IC50 = 5 μM	20056548
HepG2	Antiproliferative activity assay	IC50 = 5 μM	23260578
HepG2	Antiproliferative activity assay	IC50 = 5 μM	23932071
NCI-H23	Growth inhibition assay	TGI = 5.01 μM	28088086
NCI-H322M	Growth inhibition assay	TGI = 5.01 μM	28088086
NCI-H460	Growth inhibition assay	TGI = 5.01 μM	28088086
NCI-H522	Growth inhibition assay	TGI = 5.01 μM	28088086
HT-29	Growth inhibition assay	TGI = 5.01 μM	28088086
CCRF-CEM	Growth inhibition assay	TGI = 5.01 μM	28088086
SW620	Growth inhibition assay	TGI = 5.01 μM	28088086
HOP92	Growth inhibition assay	TGI = 5.01 μM	28088086
786-0	Growth inhibition assay	TGI = 5.01 μM	28088086
MDA-MB-435	Growth inhibition assay	TGI = 5.01 μM	28088086
PC3	Growth inhibition assay	TGI = 5.01 μM	28088086
UACC257	Growth inhibition assay	TGI = 5.01 μM	28088086
SKOV3	Growth inhibition assay	TGI = 5.01 μM	28088086
RXF393	Growth inhibition assay	TGI = 5.01 μM	28088086
T47D	Growth inhibition assay	TGI = 5.01 μM	28088086
MDA-MB-468	Growth inhibition assay	TGI = 5.01 μM	28088086
UACC62	Antiproliferative activity assay	TGI = 5.01 μM	27017549
UACC257	Antiproliferative activity assay	TGI = 5.01 μM	27017549
SK-MEL-5	Antiproliferative activity assay	LC50 = 5.01 μM	27017549
M14	Antiproliferative activity assay	TGI = 5.01 μM	27017549
NCI-H23	Antiproliferative activity assay	TGI = 5.01 μM	27017549
SF295	Antiproliferative activity assay	TGI = 5.01 μM	27017549
HOP92	Antiproliferative activity assay	TGI = 5.01 μM	27017549
BT549	Antiproliferative activity assay	TGI = 5.01 μM	27017549
MDA-MB-231	Cytotoxicity assay	IC50 = 5.1 μM	26159483
DU145	Cytotoxicity assay	IC50 = 5.1 μM	22708987
A549	Cytotoxicity assay	IC50 = 5.21 μM	20181414
HeLa	Cytotoxicity assay	IC50 = 5.23 μM	26342867
786-O	Cytotoxicity assay	IC50 = 5.3 μM	29786436
HCT116	Antiproliferative activity assay	GI50 = 5.4 μM	15225706
A375	Antiproliferative activity assay	IC50 = 5.4 μM	18477505
SK-MEL-188	Antiproliferative activity assay	IC50 = 5.4 μM	17561392
A375	Antiproliferative activity assay	IC50 = 5.4 μM	20056548
MCF7	Cytotoxicity assay	IC50 = 5.5 μM	26159483
A375	Antiproliferative activity assay	IC50 = 5.58 μM	19464887
A375P	Cytotoxicity assay	IC50 = 5.58 μM	20797858
A375P	Antiproliferative activity assay	GI50 = 5.58 μM	21353571
A375P	Growth inhibition assay	GI50 = 5.58 μM	22014755
A375P	Growth inhibition assay	GI50 = 5.58 μM	20149658
A375P	Antiproliferative activity assay	GI50 = 5.58 μM	20466542
A375P	Antiproliferative activity assay	IC50 = 5.6 μM	19857963
A375P	Antiproliferative activity assay	IC50 = 5.6 μM	21592628
A375P	Antiproliferative activity assay	IC50 = 5.6 μM	22033063
A375P	Cytotoxicity assay	IC50 = 5.6 μM	19897366
A375P	Antiproliferative activity assay	IC50 = 5.6 μM	22647720
HCT116	Cytotoxicity assay	IC50 = 5.65 μM	24215818
SH-SY5Y	Antiproliferative activity assay	IC50 = 5.73 μM	24315192
HepG2	Cytotoxicity assay	IC50 = 5.74 μM	25461318
Bel7402	Cytotoxicity assay	IC50 = 5.8 μM	23454017
HT-29	Cytotoxicity assay	IC50 = 5.9 μM	28865276
melanoma	Growth inhibition assay	IC50 = 6.1 μM	16392826
K562	Antiproliferative activity assay	GI50 = 6.2 μM	21708468
HepG2	Cytotoxicity assay	IC50 = 6.2 μM	28865276
A549	Anticancer activity assay	IC50 = 6.21 μM	29549841
SMMC7721	Antiproliferative activity assay	IC50 = 6.23 μM	22721924
HepG2	Antiproliferative activity assay	IC50 = 6.3 μM	23932071
SF295	Growth inhibition assay	TGI = 6.31 μM	28088086
SK-MEL-2	Growth inhibition assay	TGI = 6.31 μM	28088086
OVCAR5	Growth inhibition assay	TGI = 6.31 μM	28088086
UO31	Growth inhibition assay	TGI = 6.31 μM	28088086
A498	Antiproliferative activity assay	TGI = 6.31 μM	27017549
MALME-3M	Antiproliferative activity assay	TGI = 6.31 μM	27017549
U251	Antiproliferative activity assay	TGI = 6.31 μM	27017549
SK-MEL-2	Antiproliferative activity assay	LC50 = 6.31 μM	27017549
RPMI8226	Antiproliferative activity assay	TGI = 6.31 μM	27017549
HCC2998	Antiproliferative activity assay	LC50 = 6.31 μM	27017549
NCI-H522	Antiproliferative activity assay	TGI = 6.31 μM	27017549
HUVEC	Antiproliferative activity assay	IC50 = 6.42 μM	23644219
A549	Cytotoxicity assay	IC50 = 6.53 μM	27043268
A549	Cytotoxicity assay	IC50 = 6.53 μM	28340913
LoVo	Antiproliferative activity assay	IC50 = 6.56 μM	24315192
A375	Function assay	IC50 = 6.599 μM	21807507
HCT116	Function assay	GI50 = 6.6 μM	15225706
HepG2	Cytotoxicity assay	IC50 = 6.7 μM	26159483
BCPAP	Antiproliferative activity assay	IC50 = 6.7 μM	29032031
A549	Cytotoxicity assay	IC50 = 6.7 μM	28865276
PC3	Cytotoxicity assay	IC50 = 6.8 μM	23021967
SGC7901	Cytotoxicity assay	IC50 = 6.9 μM	23454017
OS-RC2	Cytotoxicity assay	IC50 = 7 μM	29517908
OS-RC2	Cytotoxicity assay	IC50 = 7 μM	29297688
COLO205	Antiproliferative activity human	IC50 = 7.04 μM	28242553
rhabdomyosarcoma	Cytotoxicity activity against human	CC50 = 7.05 μM	27288186
HuH7	Cytotoxicity assay	IC50 = 7.1 μM	26159483
MDA-MB-231	Antiproliferative activity assay	IC50 = 7.18 μM	22721924
FLT3-negative K562	Cytotoxicity assay	GI50 = 7.3 μM	23618709
K562	Function assay	GI50 = 7.3 μM	26081023
K562	Function assay	GI50 = 7.3 μM	26081023
MCF7	Antiproliferative activity assay	IC50 = 7.33 μM	23644219
A549	Cytotoxicity assay	TGI = 7.36 μM	26590508
WI38	Cytotoxicity assay	IC50 = 7.54 μM	24826815
A375	Cytotoxicity assay	IC50 = 7.56 μM	24215818
MDA-MB-231	Cytotoxicity assay	IC50 = 7.62 μM	20181414
786-0	Cytotoxicity assay	TGI = 7.62 μM	26590508
HS27	Antiproliferative activity assay	IC50 = 7.8 μM	19857963
HS27	Cytotoxicity assay	IC50 = 7.8 μM	19897366
HCT116	Cytotoxicity assay	IC50 = 7.8 μM	22483592
HS27	Antiproliferative activity assay	IC50 = 7.85 μM	19464887
HS27	Antiproliferative activity assay	GI50 = 7.85 μM	21353571
A549/ATCC	Growth inhibition assay	TGI = 7.94 μM	28088086
DU145	Growth inhibition assay	TGI = 7.94 μM	28088086
NCI/ADR-RES	Growth inhibition assay	TGI = 7.94 μM	28088086
MCF7	Growth inhibition assay	TGI = 7.94 μM	28088086
PC3	Antiproliferative activity assay	TGI = 7.94 μM	27017549
UO31	Antiproliferative activity assay	TGI = 7.94 μM	27017549
NCI-ADR-RES	Antiproliferative activity assay	TGI = 7.94 μM	27017549
LOXIMVI	Antiproliferative activity assay	LC50 = 7.94 μM	27017549
SK-MEL-28	Antiproliferative activity assay	TGI = 7.94 μM	27017549
KM12	Antiproliferative activity assay	TGI = 7.94 μM	27017549
COLO205	Antiproliferative activity assay	TGI = 7.94 μM	27017549
HT-29	Antiproliferative activity assay	TGI = 7.94 μM	27017549
NCI-H226	Antiproliferative activity assay	TGI = 7.94 μM	27017549
HOP62	Antiproliferative activity assay	TGI = 7.94 μM	27017549
T47D	Antiproliferative activity assay	TGI = 7.94 μM	27017549
MDA-MB-468	Antiproliferative activity assay	TGI = 7.94 μM	27017549
EKVX	Antiproliferative activity assay	TGI = 7.94 μM	27017549
MCF7	Antiproliferative activity assay	TGI = 7.94 μM	27017549
Hs 578T	Antiproliferative activity assay	TGI = 7.94 μM	27017549
MGC803	Antiproliferative activity assay	IC50 = 7.99 μM	26560049
HCT116	Antiproliferative activity assay	IC50 = 8.08 μM	24440479
PC3	Cytotoxicity assay	IC50 = 8.08 μM	27043268
HCT116	Antiproliferative activity assay	IC50 = 8.08 μM	23644219
WM266.4	Antiproliferative activity assay	GI50 = 8.1 μM	23025996
WM266.4	Antiproliferative activity assay	GI50 = 8.12 μM	22583669
Ketr3	Antiproliferative activity assay	IC50 = 8.27 μM	30216849
A375	Antiproliferative activity assay	IC50 = 8.27 μM	30216849
HepG2	Antiproliferative activity assay	IC50 = 8.27 μM	30216849
MX1	Antiproliferative activity assay	IC50 = 8.27 μM	30216849
MX1	Cytotoxicity assay	IC50 = 8.27 μM	24675135
WM266.4	Growth inhibition assay	GI50 = 8.3 μM	22361686
PLC/PRF/5	Cytotoxicity assay	IC50 = 8.3 μM	21531053
A375	Antiproliferative activity assay	IC50 = 8.33 μM	29886324
HCT116	Cytotoxicity assay	IC50 = 8.41 μM	29631788
WI38	Cytotoxicity assay	IC50 = 8.42 μM	26991938
HepG2	Cytotoxicity assay	IC50 = 8.42 μM	27162123
HepG2	Cytotoxicity assay	IC50 = 8.42 μM	23871909
HT-29	Antiproliferative activity assay	IC50 = 8.44 μM	29602674
HepG2	Cytotoxicity assay	IC50 = 8.67 μM	24675135
MCF7	Cytotoxicity assay	IC50 = 8.83 μM	20435479
MCF7	Cytotoxicity assay	IC50 = 9.12 μM	24300920
HepG2	Antiproliferative activity assay	IC50 = 9.14 μM	26560049
A375	Cytotoxicity assay	IC50 = 9.17 μM	24675135
MGC803	Antiproliferative activity assay	IC50 = 9.2 μM	29032031
SKOV3	Cytotoxicity assay	IC50 = 9.25 μM	24300920
RS4:11	Function assay	GI50 = 9.3 μM	26081023
RS4:11	Cytotoxicity assay	GI50 = 9.3 μM	23618709
MIAPaCa2	Antiproliferative activity assay	IC50 = 9.32 μM	29032031
PANC1	Growth inhibition assay	IC50 = 9.32 μM	29102175
MHCC97H	Growth inhibition assay	IC50 = 9.32 μM	29102175
RS4:11	Antiproliferative activity assay	GI50 = 9.4 μM	21708468
Hep3B	Cytotoxicity assay	IC50 = 9.4 μM	28865276
LoVo	Growth inhibition assay	IC50 = 9.47 μM	29102175
SMMC7721	Antiproliferative activity assay	IC50 = 9.96 μM	25637123
MCF7	Cytotoxicity assay	TGI = 9.97 μM	26590508
IGROV1	Growth inhibition assay	TGI = 10 μM	28088086
ACHN	Growth inhibition assay	TGI = 10 μM	28088086
TK10	Growth inhibition assay	TGI = 10 μM	28088086
786-0	Antiproliferative activity assay	TGI = 10 μM	27017549
SN12C	Antiproliferative activity assay	TGI = 10 μM	27017549
Caki1	Antiproliferative activity assay	LC50 = 10 μM	27017549
TK10	Antiproliferative activity assay	TGI = 10 μM	27017549
RXF393	Antiproliferative activity assay	TGI = 10 μM	27017549
OVCAR8	Antiproliferative activity assay	TGI = 10 μM	27017549
SNB75	Antiproliferative activity assay	TGI = 10 μM	27017549
NCI-H322M	Antiproliferative activity assay	TGI = 10 μM	27017549
MDA-MB-435	Antiproliferative activity assay	LC50 = 10 μM	27017549
SF539	Antiproliferative activity assay	TGI = 10 μM	27017549
SF268	Antiproliferative activity assay	TGI = 10 μM	27017549
NCI-H460	Antiproliferative activity assay	TGI = 10 μM	27017549
DU145	Antiproliferative activity assay	TGI = 10 μM	27017549
K1	Antiproliferative activity assay	IC50 = 10.2 μM	29032031
Bel7402	Cytotoxicity assay	IC50 = 10.26 μM	21504204
Bel7402	Growth inhibition assay	IC50 = 10.31 μM	29102175
OVCAR3	Cytotoxicity assay	TGI = 10.32 μM	26590508
SGC7901	Cytotoxicity assay	IC50 = 10.37 μM	20435479
SNB75	Cytotoxicity assay	TGI = 10.42 μM	26590508
A431	Antiproliferative activity assay	IC50 = 10.46 μM	29032031
SMMC7721	Antiproliferative activity assay	IC50 = 10.61 μM	29032031
GES-1	Cytotoxicity assay	IC50 = 10.68 μM	27162123
H460	Cytotoxicity assay	IC50 = 10.8 μM	24300920
BGC823	Antiproliferative activity assay	IC50 = 10.91 μM	22721924
Hep3B	Cytotoxicity assay	IC50 = 11.2 μM	28342400
MCF7	Cytotoxicity assay	IC50 = 11.34 μM	27162123
MCF7	Cytotoxicity assay	IC50 = 11.34 μM	23871909
SK-MEL-2	Antiproliferative activity human	IC50 = 11.35 μM	28242553
HepG2	Cytotoxicity assay	IC50 = 11.49 μM	21504204
A375P	Antiproliferative activity assay	IC50 = 11.5 μM	22014559
SGC7901	Cytotoxicity assay	IC50 = 11.5 μM	24300920
HeLa	Antiproliferative activity assay	IC50 = 12.01 μM	29103873
PANC1	Cytotoxicity assay	IC50 = 12.3 μM	24300920
HepG2	Antiproliferative activity assay	IC50 = 12.54 μM	29032031
A549	Antiproliferative activity assay	IC50 = 12.54 μM	23644219
Caki1	Growth inhibition assay	TGI = 12.59 μM	28088086
OVCAR8	Growth inhibition assay	TGI = 12.59 μM	28088086
SKOV3	Antiproliferative activity assay	TGI = 12.6 μM	27017549
ACHN	Antiproliferative activity assay	TGI = 12.6 μM	27017549
OVCAR3	Antiproliferative activity assay	TGI = 12.6 μM	27017549
OVCAR4	Antiproliferative activity assay	TGI = 12.6 μM	27017549
HCT15	Antiproliferative activity assay	TGI = 12.6 μM	27017549
SW620	Antiproliferative activity assay	TGI = 12.6 μM	27017549
A549/ATCC	Antiproliferative activity assay	TGI = 12.6 μM	27017549
MDA-MB-468	Cytotoxicity assay	TGI = 13.09 μM	26590508
SK-MEL-28	Cytotoxicity assay	TGI = 13.39 μM	26590508
A549	Antiproliferative activity assay	IC50 = 13.64 μM	26560049
A375	Antiproliferative activity human	IC50 = 13.64 μM	28242553
A375	Antiproliferative activity assay	IC50 = 13.64 μM	25462267
K562	Antiproliferative activity assay	IC50 = 13.85 μM	23644219
Hep3B	Cytotoxicity assay	IC50 = 14.08 μM	21504204
T47D	Cytotoxicity assay	TGI = 14.38 μM	26590508
NCI-H226	Cytotoxicity assay	TGI = 14.42 μM	26590508
MDA-MB-231	Antiproliferative activity assay	IC50 = 14.62 μM	24440479
MDA-MB-231	Antiproliferative activity assay	IC50 = 14.62 μM	23644219
NCI-H522	Cytotoxicity assay	TGI = 14.82 μM	26590508
SK-MEL-2	Cytotoxicity assay	TGI = 14.85 μM	26590508
OS-RC2	Cytotoxicity assay	IC50 = 15 μM	29786436
HepG2	Antiproliferative activity assay	IC50 = 15 μM	29103873
fibroblast	Antiproliferative activity assay	IC50 = 15.1 μM	18477505
HT-29	Cytotoxicity assay	IC50 = 15.2 μM	24675135
U87MG	Cytotoxicity assay	IC50 = 15.57 μM	24826815
BT549	Antiproliferative activity assay	LC50 = 15.8 μM	27017549
GES-1	Cytotoxicity assay	IC50 = 15.8 μM	23871909
SNB19	Antiproliferative activity assay	TGI = 15.85 μM	27017549
IGROV1	Antiproliferative activity assay	TGI = 15.9 μM	27017549
HCT116	Antiproliferative activity assay	LC50 = 15.9 μM	27017549
OS-RC2	Cytotoxicity assay	IC50 = 16 μM	23454017
A375	Cytotoxicity assay	IC50 = 16.24 μM	25461318
SKOV3	Cytotoxicity assay	TGI = 16.36 μM	26590508
WM1361	Antiproliferative activity assay	IC50 = 16.44 μM	29602674
MKN28	Antiproliferative activity assay	IC50 = 17 μM	29032031
SMMC7721	Cytotoxicity assay	IC50 = 17.3 μM	21504204
UACC257	Cytotoxicity assay	TGI = 17.33 μM	26590508
EAhy926	Antiangiogenic activity assay	IC50 = 18.52 μM	29032031
SMMC7721	Cytotoxicity assay	IC50 = 18.7 μM	24300920
Ketr3	Cytotoxicity assay	IC50 = 18.8 μM	24675135
NCI-H522	Cytotoxicity assay	IC50 = 19.26 μM	25461318
A549	Cytotoxicity assay	IC50 = 19.54 μM	27162123
SH-SY5Y	Cytotoxicity assay	IC50 = 19.54 μM	23871909
MGC803	Antiproliferative activity assay	IC50 = 19.92 μM	29103873
EKVX	Growth inhibition assay	TGI = 19.95 μM	28088086
OVCAR5	Antiproliferative activity assay	TGI = 20 μM	27017549
UACC62	Antiproliferative activity assay	LC50 = 20 μM	27017549
UACC257	Antiproliferative activity assay	LC50 = 20 μM	27017549
MDA-MB-231	Antiproliferative activity assay	LC50 = 20 μM	27017549
U87	Cytotoxicity assay	IC50 = 21.07 μM	20435479
EJ	Cytotoxicity assay	IC50 = 22.9 μM	24300920
HCT116	Antiproliferative activity assay	IC50 = 23.31 μM	29602674
HOP62	Cytotoxicity assay	TGI = 23.55 μM	26590508
MDA-MB-231	Cytotoxicity assay	TGI = 23.93 μM	26590508
PC3	Antiproliferative activity assay	IC50 = 24.2 μM	24440479
PC3	Antiproliferative activity assay	IC50 = 24.2 μM	23644219
EAhy926	Antiproliferative activity assay	IC50 = 24.36 μM	28068599
EAhy926	Anti-angiogenic activity in human	IC50 = 24.36 μM	29102175
U251	Cytotoxicity assay	IC50 = 24.71 μM	20435479
NIH/3T3	Antiproliferative activity assay	IC50 = 24.75 μM	21592628
NIH/3T3	Antiproliferative activity assay	IC50 = 24.75 μM	22647720
DU145	Cytotoxicity assay	IC50 = 24.91 μM	27162123
DU145	Cytotoxicity assay	IC50 = 24.91 μM	23871909
U251	Antiproliferative activity assay	LC50 = 25.1 μM	27017549
M14	Antiproliferative activity assay	LC50 = 25.1 μM	27017549
NCI-H522	Antiproliferative activity assay	LC50 = 25.1 μM	27017549
OVCAR4	Growth inhibition assay	TGI = 25.12 μM	28088086
SH-SY5Y	Cytotoxicity assay	IC50 = 27.71 μM	27162123
A549	Cytotoxicity assay	IC50 = 27.71 μM	23871909
PLC/PRF/5	Cytotoxicity assay	IC50 = 29.9 μM	28109948
SK-MEL-5	Cytotoxicity assay	TGI = 31.26 μM	26590508
A498	Antiproliferative activity assay	LC50 = 31.6 μM	27017549
SK-MEL-28	Antiproliferative activity assay	LC50 = 31.6 μM	27017549
KM12	Antiproliferative activity assay	LC50 = 31.6 μM	27017549
COLO205	Antiproliferative activity assay	LC50 = 31.6 μM	27017549
NCI-H226	Antiproliferative activity assay	LC50 = 31.6 μM	27017549
SF295	Antiproliferative activity assay	LC50 = 31.6 μM	27017549
HOP62	Antiproliferative activity assay	LC50 = 31.6 μM	27017549
T47D	Antiproliferative activity assay	LC50 = 31.6 μM	27017549
MHCC97L	Cytotoxicity assay	IC50 = 34.41 μM	28109948
MDA-MB-231	Antiproliferative activity assay	IC50 = 35 μM	24315192
MDA-MB-231	Cytotoxicity assay	IC50 = 36 μM	22483592
B16-BL6	Cytotoxicity assay	IC50 = 36.48 μM	29631788
UO31	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
SN12C	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
RXF393	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
SNB75	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
SF268	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
NCI-H23	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
HT-29	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
HOP92	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
NCI-H460	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
SW620	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
MDA-MB-468	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
MALME-3M	Growth inhibition assay	TGI = 39.81 μM	28088086
点击查看更多细胞系数据

生物活性

产品描述

靶点

Raf-1 ^[1] (Cell-free assay)	mVEGFR2(Flk1) ^[1] (Cell-free assay)	mVEGFR3 ^[1] (Cell-free assay)	B-Raf ^[1] (Cell-free assay)	B-Raf (V599E) ^[1] (Cell-free assay)	点击更多
6 nM	15 nM	20 nM	22 nM	38 nM	点击更多

体外研究(In Vitro)
体外研究活性	Sorafenib抑制野生型和V599E突变型B-Raf活性，IC50分别为22 nM 和 38 nM。Sorafenib也能有效抑制mVEGFR2 (Flk-1)，mVEGFR3，mPDGFRβ，Flt3，和c-Kit，IC50分别为15 nM，20 nM，57 nM，58 nM，和68 nM。Sorafenib 能够较弱地抑制FGFR-1，IC50 为580 nM。Sorafenib对ERK-1，MEK-1，EGFR，HER-2，IGFR-1，c-Met，PKB，PKA，cdk1/cyclinB，PKCα，PKCγ，和pim-1没有活性。Sorafenib显著抑制NIH 3T3细胞中VEGFR2磷酸化，IC50 为 30 nM，也会抑制HEK-293细胞中Flt-3磷酸化，IC50 为20 nM。Sorafenib有效阻断大多数细胞中MEK 1/2 和 ERK 1/2磷酸化，但不阻断A549 或 H460细胞中该过程，同时不影响PKB通路的抑制。Sorafenib抑制HAoSMC 和 MDA-MB-231细胞的增殖，IC50分别为0.28 μM 和 2.6 μM。^[1]除了抑制RAF/MEK/ERK信号通路，Sorafenib tosylate显著抑制eIF4E的磷酸化作用，并以MEK/ERK依赖的方式下调肝癌(HCC)细胞中Mcl-1水平。Sorafenib 抑制PLC/PRF/5 和HepG2细胞的增殖，IC50分别为6.3 μM 和 4.5 μM，并诱导显著的细胞凋亡。^[2]
激酶实验	生化检测
激酶实验	重组杆状病毒表达的Raf-1 (残基305–648)和 B-Raf (残基 409–765)以融合蛋白纯化。全长人MEK-1由PCR产生，并以大肠杆菌裂解物中的融合蛋白纯化。将Sorafenib加入到含Raf-1 (80纳克)，或B-Raf (80 纳克) 以及MEK-1 (1 微克) 混合物的实验缓冲液[20 mM Tris (pH 8.2)，100 mM NaCl，5 mM MgCl₂，和0.15% β-巯基乙醇]中，DMSO终浓度为1%。加入25微升10 μM γ[³³P]ATP (400 Ci/mol)启动Raf激酶试验(终体积50微升)，并在32 °C下培育25分钟。磷酸化的MEK-1通过过滤到磷酸纤维素板上采集，使用1%磷酸洗掉未结合的放射性。微波炉加热干燥后，使用β型板计数器量化过滤器结合放射性。人VEGFR2 (KDR)激酶域被表达，并从Sf9裂解物中纯化。VEGFR2的时间分辨荧光分析法能量转移测试在96孔不透明板中以时间分辨荧光分析法能量转移格式进行。最终反应条件如下：1 到10 μM ATP，25 nM poly GT生物素，2 nM 铕标记的磷酸(p)-酪氨酸抗体(PY20)，10 nM APC，1% DMSO 终浓度的1 到 7 nM 细胞质激酶域，50 mM HEPES (pH 7.5)，10 mM MgCl₂，0.1 mM EDTA，0.015% Brij-35，0.1 毫克/毫升BSA，和0.1% β-巯基乙醇。反应体积为100微升，加入酶启动反应。反应启动~1.5 到 2.0小时后，板以615 和 665 nM在Perkin-Elmer VictorV多标记分析仪上读数。信号按如下比率计算：对每孔(665 nm/615 nM) × 10,000。对IC50的产生，在酶起始反应之前加入Sorafenib。50倍的库存板由Sorafenib在50% DMSO/50%蒸馏水溶液中连续稀释制得。最终Sorafenib在1% DMSO中的浓度范围为10 μM 到 4.56 nM。
细胞实验	细胞系	MDA-MB-231，和 HAoSMC
	浓度	溶解于DMSO，终浓度为~10 μM
	孵育时间	72小时
	方法	细胞在逐渐增加浓度的Sorafenib下暴露72小时。细胞数通过Cell TiterGlo ATP发光测定试剂盒进行定量。该试验通过测定基于细胞中ATP量的发光信号，测量每孔中的活细胞。
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	LC3-I / LC-3II / ATG5 p-STAT3 / STAT3 / Mcl-1 β-catenin / Survivin / Mcl-1 / PTMA pERK / ERK p-PKM2(y105) / PMK2 / Caspase-9 RET(pY1016) / VEGFR2(pY1214) / MEK1(pT292) / ERK(pY204) Cyclin D1		23392173
	Growth inhibition assay	Cell viability		26039995
	Immunofluorescence	p65 cytochrome c		22286758
	ELISA	TGF-beta / CD206 Caspase-9 / Caspase-3		26158762

体内研究(In Vivo)
体内研究活性	Sorafenib(~60 mg/kg)口服给药，对各种人肿瘤异种移植模型，包括MDA-MB-231，Colo-205，HT-29，DLD-1，NCI-H460，和A549表现出广谱的、剂量依赖性抗肿瘤活性，而没有毒性。与抗肿瘤功效相联系，Sorafenib 治疗有效抑制HT-29 和 MDA-MB-231异种移植物中MEK 1/2磷酸化和pERK 1/2水平，但对Colo-205异种移植物没有作用，并且也能显著抑制MDA MB-231，HT-29 和 Colo-205肿瘤异种移植物中肿瘤微血管面积(MVA)和微血管密度(MVD)。^[1] 在SCID小鼠体内，Sorafenib治疗对PLC/PRF/5肿瘤异种移植产生剂量依赖性生长抑制，10 mg/kg和30 mg/kg剂量下，TGIs分别为49%和78%，与ERK 和 eIF4E磷酸化抑制，微血管面积减少，和肿瘤细胞凋亡的诱导相一致。^[2] Sorafenib通过下调NF-κB介导的Mcl-1 和 cIAP2表达的作用机制使bax^-/-细胞对TRAIL剂量依赖性敏感。 Sorafenib (30-60 mg/kg) 与 TRAIL (5 mg/kg)结合对TRAIL抗性HCT116 bax^-/-和HT29肿瘤异种移植物表现出显著的功效。^[3]
动物实验	Animal Models	雌性 NCr-nu/nu 小鼠，皮下植入MDA-MB-231，Colo-205，HT-29，H460，或 A549 细胞
	Dosages	~60 mg/kg
	Administration	口服，每天一次

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05068752	Recruiting	Pancreas Cancer	HonorHealth Research Institute\|Bayer\|Genentech Inc.	October 28 2021	Phase 2
NCT04763408	Active not recruiting	Carcinoma Hepatocellular	Eisai Inc.	April 9 2021	--

参考文献
https://pubmed.ncbi.nlm.nih.gov/15466206/ https://pubmed.ncbi.nlm.nih.gov/17178882/ https://pubmed.ncbi.nlm.nih.gov/17613437/

参考文献

https://pubmed.ncbi.nlm.nih.gov/15466206/
https://pubmed.ncbi.nlm.nih.gov/17178882/
https://pubmed.ncbi.nlm.nih.gov/17613437/

化学信息&溶解度

分子量	464.82	分子式	C₂₁H₁₆ClF₃N₄O₃
CAS号	284461-73-0	SDF	Download Sorafenib SDF
Smiles	CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 93 mg/mL ( (200.07 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 92 mg/mL ( (197.92 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 120 mg/mL ( (258.16 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 93 mg/mL ( (200.07 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解配方批次：现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂				动物体内配方计算器
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 Corn oil 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	5.000mg/ml (10.76mM)	以 1 mL 工作液为例，取50μL100mg/ml的澄清DMSO储备液加到950μL玉米油中，混合均匀。工作液请现配现用！
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 45%PEG400 2 50%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	0.380mg/ml (0.82mM)	以 1 mL 工作液为例，取50μL7.5mg/ml的澄清DMSO储备液加到450μL PEG 400中，混合均匀使其澄清；然后继续加入500μL ddH2O定容至 1 mL。工作液请现配现用！
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	2.500mg/ml (5.38mM)	以 1 mL 工作液为例,取50μL50mg/ml的澄清DMSO储备液加到400μLPEG300中,混合均匀使其澄清;向上述体系中加入50μLTween80,混合均匀使其澄清;然后继续加入500μLddH2O定容至1mL。工作液请现配现用!
澄清溶液	5% DMSO 1 95% Corn oil 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	0.500mg/ml (1.08mM)	以1 mL工作液为例，取50μL 10mg/ml的澄清DMSO储备液加到950μL玉米油中，混合均匀。工作液请现配现用！
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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操作手册

如果有其他问题，请给我们留言。

* 必填项

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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