Axitinib

别名: AG 013736 中文名称:阿西替尼,阿昔替尼

Axitinib是一种多靶点抑制剂,作用于 VEGFR1VEGFR2VEGFR3,PDGFRβ和c-Kit,在猪主动脉内皮细胞中IC50分别为0.1 nM,0.2 nM,0.1-0.3 nM,1.6 nM和1.7 nM。

Axitinib Chemical Structure

Axitinib Chemical Structure

CAS: 319460-85-0

规格 价格 库存 购买数量
10mM (1mL in DMSO) 647.01 现货
50mg 570.91 现货
100mg 975.25 现货
1g 4013.1 现货
更大包装 有超大折扣

400-668-6834

info@selleck.cn

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Axitinib相关产品

相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
MCF7 Antiproliferative assay 5 days Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 0.97 μM. 23829549
MDA-MB-468 Antiproliferative assay 5 days Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 1.3 μM. 23829549
HCC1954 Antiproliferative assay 5 days Antiproliferative activity against human HCC1954 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 2.7 μM. 23829549
SKBR3 Antiproliferative assay 5 days Antiproliferative activity against human SKBR3 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 3.8 μM. 23829549
MDA-MB-231 Antiproliferative assay 5 days Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 7.3 μM. 23829549
MCF7 Cytotoxicity assay 5 days Cytotoxicity against human MCF7 cells after 5 days by SRB assay, GI50 = 2.3 μM. 24867403
MDA-MB-468 Cytotoxicity assay 5 days Cytotoxicity against human MDA-MB-468 cells after 5 days by SRB assay, GI50 = 2.8 μM. 24867403
SKBR3 Cytotoxicity assay 5 days Cytotoxicity against human SKBR3 cells after 5 days by SRB assay, GI50 = 4.6 μM. 24867403
MDA-MB-231 Cytotoxicity assay 5 days Cytotoxicity against human MDA-MB-231 cells after 5 days by SRB assay, GI50 = 11 μM. 24867403
HUVEC Antiproliferative assay 1 hr Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as reduction in cell viability preincubated for 1 hr followed by addition of VEGF measured after 72 hrs by MTT assay, IC50 = 0.0005 μM. ChEMBL
HUVEC Antiproliferative assay 1 hr Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as reduction in cell viability preincubated for 1 hr followed by addition of VEGF measured after 72 hrs in presence of albumin by MTT assay, IC50 = 0.0027 μM. ChEMBL
A549 Antiproliferative assay 48 hrs Antiproliferative activity against VEGF-stimulated human A549 cells after 48 hrs by CCK8 assay, IC50 = 22.4 μM. ChEMBL
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against VEGF-stimulated human HepG2 cells after 48 hrs by CCK8 assay, IC50 = 38.7 μM. ChEMBL
HEC-1 Growth Inhibition Assay IC50=8.78439 μM SANGER
8505C Growth Inhibition Assay IC50=8.64824 μM SANGER
NOS-1 Growth Inhibition Assay IC50=8.51534 μM SANGER
TE-1 Growth Inhibition Assay IC50=8.44316 μM SANGER
D-423MG Growth Inhibition Assay IC50=8.2172 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=8.15783 μM SANGER
COLO-800 Growth Inhibition Assay IC50=7.94492 μM SANGER
MDA-MB-415 Growth Inhibition Assay IC50=7.89186 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=7.6961 μM SANGER
IA-LM Growth Inhibition Assay IC50=7.68613 μM SANGER
SW1088 Growth Inhibition Assay IC50=7.65826 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=7.64934 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=7.63033 μM SANGER
HCC2998 Growth Inhibition Assay IC50=7.60743 μM SANGER
HAL-01 Growth Inhibition Assay IC50=7.60644 μM SANGER
HCC1419 Growth Inhibition Assay IC50=7.53 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=7.4815 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=7.32386 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=7.2072 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=7.19345 μM SANGER
SNU-449 Growth Inhibition Assay IC50=7.01072 μM SANGER
OC-314 Growth Inhibition Assay IC50=6.91159 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=6.54572 μM SANGER
HCC1569 Growth Inhibition Assay IC50=6.53737 μM SANGER
S-117 Growth Inhibition Assay IC50=6.50267 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=6.41688 μM SANGER
D-502MG Growth Inhibition Assay IC50=6.28857 μM SANGER
MKN45 Growth Inhibition Assay IC50=6.26016 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=6.11248 μM SANGER
NCI-H1048 Growth Inhibition Assay IC50=6.10599 μM SANGER
A704 Growth Inhibition Assay IC50=6.10574 μM SANGER
OAW-42 Growth Inhibition Assay IC50=5.98821 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=5.92771 μM SANGER
KM-H2 Growth Inhibition Assay IC50=5.92395 μM SANGER
COLO-829 Growth Inhibition Assay IC50=5.91504 μM SANGER
NCI-H28 Growth Inhibition Assay IC50=5.87918 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=5.84325 μM SANGER
EW-16 Growth Inhibition Assay IC50=5.75583 μM SANGER
JVM-3 Growth Inhibition Assay IC50=5.72325 μM SANGER
D-392MG Growth Inhibition Assay IC50=5.57849 μM SANGER
EFM-19 Growth Inhibition Assay IC50=5.41737 μM SANGER
NCI-H1155 Growth Inhibition Assay IC50=5.38185 μM SANGER
KM12 Growth Inhibition Assay IC50=5.29827 μM SANGER
NBsusSR Growth Inhibition Assay IC50=5.03514 μM SANGER
CAS-1 Growth Inhibition Assay IC50=4.99908 μM SANGER
A3-KAW Growth Inhibition Assay IC50=4.97352 μM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=4.89048 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=4.81418 μM SANGER
HOS Growth Inhibition Assay IC50=4.6977 μM SANGER
SNU-423 Growth Inhibition Assay IC50=4.6079 μM SANGER
SW1573 Growth Inhibition Assay IC50=4.55163 μM SANGER
EW-1 Growth Inhibition Assay IC50=4.53014 μM SANGER
Hs-578-T Growth Inhibition Assay IC50=4.31468 μM SANGER
HGC-27 Growth Inhibition Assay IC50=4.2966 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=4.26658 μM SANGER
CAL-27 Growth Inhibition Assay IC50=4.24344 μM SANGER
ONS-76 Growth Inhibition Assay IC50=4.24192 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=4.22177 μM SANGER
HCC1187 Growth Inhibition Assay IC50=4.21597 μM SANGER
JEG-3 Growth Inhibition Assay IC50=4.15916 μM SANGER
DU-145 Growth Inhibition Assay IC50=4.12825 μM SANGER
HCC1395 Growth Inhibition Assay IC50=3.99484 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=3.99126 μM SANGER
ABC-1 Growth Inhibition Assay IC50=3.93911 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=3.91808 μM SANGER
ES1 Growth Inhibition Assay IC50=3.83094 μM SANGER
COR-L105 Growth Inhibition Assay IC50=3.63334 μM SANGER
EW-11 Growth Inhibition Assay IC50=3.63022 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=3.62616 μM SANGER
SCC-4 Growth Inhibition Assay IC50=3.50396 μM SANGER
ES8 Growth Inhibition Assay IC50=3.34999 μM SANGER
SW982 Growth Inhibition Assay IC50=3.33875 μM SANGER
SF126 Growth Inhibition Assay IC50=3.30017 μM SANGER
HCC1806 Growth Inhibition Assay IC50=3.27657 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=3.22805 μM SANGER
NCI-H1563 Growth Inhibition Assay IC50=3.15005 μM SANGER
SF295 Growth Inhibition Assay IC50=3.02597 μM SANGER
DMS-273 Growth Inhibition Assay IC50=2.90207 μM SANGER
CHP-212 Growth Inhibition Assay IC50=2.82091 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=2.70299 μM SANGER
DMS-114 Growth Inhibition Assay IC50=2.66345 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=2.59169 μM SANGER
GOTO Growth Inhibition Assay IC50=2.53013 μM SANGER
T-24 Growth Inhibition Assay IC50=2.48037 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=2.47168 μM SANGER
HuH-7 Growth Inhibition Assay IC50=2.42165 μM SANGER
L-363 Growth Inhibition Assay IC50=2.28061 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=2.24957 μM SANGER
ACN Growth Inhibition Assay IC50=2.23875 μM SANGER
DK-MG Growth Inhibition Assay IC50=2.23834 μM SANGER
YH-13 Growth Inhibition Assay IC50=2.21671 μM SANGER
HCE-T Growth Inhibition Assay IC50=2.20598 μM SANGER
A172 Growth Inhibition Assay IC50=2.13606 μM SANGER
RT-112 Growth Inhibition Assay IC50=2.13424 μM SANGER
GCT Growth Inhibition Assay IC50=2.00916 μM SANGER
HSC-4 Growth Inhibition Assay IC50=1.93839 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=1.86281 μM SANGER
PA-1 Growth Inhibition Assay IC50=1.82725 μM SANGER
UACC-257 Growth Inhibition Assay IC50=1.82163 μM SANGER
ALL-PO Growth Inhibition Assay IC50=1.80015 μM SANGER
HMV-II Growth Inhibition Assay IC50=1.70488 μM SANGER
NCI-H292 Growth Inhibition Assay IC50=1.66383 μM SANGER
SW780 Growth Inhibition Assay IC50=1.65158 μM SANGER
NKM-1 Growth Inhibition Assay IC50=1.60556 μM SANGER
BT-549 Growth Inhibition Assay IC50=1.56909 μM SANGER
LXF-289 Growth Inhibition Assay IC50=1.43996 μM SANGER
D-566MG Growth Inhibition Assay IC50=1.40683 μM SANGER
NCI-H1581 Growth Inhibition Assay IC50=1.39042 μM SANGER
NB10 Growth Inhibition Assay IC50=1.32557 μM SANGER
DEL Growth Inhibition Assay IC50=1.25457 μM SANGER
ES5 Growth Inhibition Assay IC50=1.17248 μM SANGER
G-402 Growth Inhibition Assay IC50=1.14694 μM SANGER
AGS Growth Inhibition Assay IC50=1.11395 μM SANGER
ES7 Growth Inhibition Assay IC50=1.11334 μM SANGER
A427 Growth Inhibition Assay IC50=1.10381 μM SANGER
AN3-CA Growth Inhibition Assay IC50=1.08389 μM SANGER
SK-OV-3 Growth Inhibition Assay IC50=1.06633 μM SANGER
H4 Growth Inhibition Assay IC50=1.06422 μM SANGER
NB14 Growth Inhibition Assay IC50=1.01801 μM SANGER
A2780 Growth Inhibition Assay IC50=1.01146 μM SANGER
SW756 Growth Inhibition Assay IC50=0.99846 μM SANGER
NEC8 Growth Inhibition Assay IC50=0.72113 μM SANGER
BE-13 Growth Inhibition Assay IC50=0.51008 μM SANGER
MFM-223 Growth Inhibition Assay IC50=0.44776 μM SANGER
MEG-01 Growth Inhibition Assay IC50=0.42361 μM SANGER
K5 Growth Inhibition Assay IC50=0.42127 μM SANGER
BV-173 Growth Inhibition Assay IC50=0.3932 μM SANGER
KG-1 Growth Inhibition Assay IC50=0.37642 μM SANGER
G-361 Growth Inhibition Assay IC50=0.32325 μM SANGER
JAR Growth Inhibition Assay IC50=0.23989 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=0.17665 μM SANGER
EM-2 Growth Inhibition Assay IC50=0.16816 μM SANGER
KU812 Growth Inhibition Assay IC50=0.16577 μM SANGER
H-EMC-SS Growth Inhibition Assay IC50=0.11005 μM SANGER
HOP-62 Growth Inhibition Assay IC50=0.10836 μM SANGER
A204 Growth Inhibition Assay IC50=0.00992 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=0.00722 μM SANGER
KASUMI-1 Growth Inhibition Assay IC50=0.00682 μM SANGER
NCI-H1703 Growth Inhibition Assay IC50=0.000902 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=0.0000513 μM SANGER
TE-11 Growth Inhibition Assay IC50=8.99551 μM SANGER
CTB-1 Growth Inhibition Assay IC50=9.01433 μM SANGER
TGBC11TKB Growth Inhibition Assay IC50=9.02241 μM SANGER
NB17 Growth Inhibition Assay IC50=9.1887 μM SANGER
Becker Growth Inhibition Assay IC50=9.41944 μM SANGER
SN12C Growth Inhibition Assay IC50=9.45234 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=9.60237 μM SANGER
D-283MED Growth Inhibition Assay IC50=9.63072 μM SANGER
D-263MG Growth Inhibition Assay IC50=9.83384 μM SANGER
MEL-JUSO Growth Inhibition Assay IC50=9.90127 μM SANGER
T98G Growth Inhibition Assay IC50=9.90203 μM SANGER
HLE Growth Inhibition Assay IC50=9.90909 μM SANGER
Ca9-22 Growth Inhibition Assay IC50=10.0665 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=10.1045 μM SANGER
T47D Growth Inhibition Assay IC50=10.155 μM SANGER
GI-1 Growth Inhibition Assay IC50=10.3533 μM SANGER
NUGC-3 Growth Inhibition Assay IC50=10.4402 μM SANGER
MDA-MB-361 Growth Inhibition Assay IC50=10.4432 μM SANGER
SCC-15 Growth Inhibition Assay IC50=10.4718 μM SANGER
KS-1 Growth Inhibition Assay IC50=10.6301 μM SANGER
CAL-12T Growth Inhibition Assay IC50=10.6361 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=10.7068 μM SANGER
HuP-T4 Growth Inhibition Assay IC50=11.0328 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=11.2657 μM SANGER
HO-1-N-1 Growth Inhibition Assay IC50=11.3398 μM SANGER
NH-12 Growth Inhibition Assay IC50=11.5378 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=11.5985 μM SANGER
K-562 Growth Inhibition Assay IC50=11.7248 μM SANGER
ES6 Growth Inhibition Assay IC50=11.8581 μM SANGER
RO82-W-1 Growth Inhibition Assay IC50=11.9064 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=11.932 μM SANGER
23132-87 Growth Inhibition Assay IC50=12.0821 μM SANGER
A549 Growth Inhibition Assay IC50=12.3285 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=12.5026 μM SANGER
H9 Growth Inhibition Assay IC50=12.5577 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=12.765 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=12.8258 μM SANGER
HSC-3 Growth Inhibition Assay IC50=12.9276 μM SANGER
PFSK-1 Growth Inhibition Assay IC50=12.9507 μM SANGER
ETK-1 Growth Inhibition Assay IC50=13.0779 μM SANGER
SW1710 Growth Inhibition Assay IC50=13.3641 μM SANGER
COLO-684 Growth Inhibition Assay IC50=13.4541 μM SANGER
RPMI-7951 Growth Inhibition Assay IC50=13.5136 μM SANGER
A101D Growth Inhibition Assay IC50=13.5349 μM SANGER
KE-37 Growth Inhibition Assay IC50=13.5887 μM SANGER
SiHa Growth Inhibition Assay IC50=13.8346 μM SANGER
NCI-H226 Growth Inhibition Assay IC50=13.8808 μM SANGER
DB Growth Inhibition Assay IC50=13.9928 μM SANGER
HT-1197 Growth Inhibition Assay IC50=14.0809 μM SANGER
SBC-5 Growth Inhibition Assay IC50=14.1362 μM SANGER
VMRC-RCZ Growth Inhibition Assay IC50=14.5774 μM SANGER
697 Growth Inhibition Assay IC50=14.627 μM SANGER
OMC-1 Growth Inhibition Assay IC50=14.7888 μM SANGER
SKG-IIIa Growth Inhibition Assay IC50=14.8001 μM SANGER
DOK Growth Inhibition Assay IC50=14.9933 μM SANGER
NCI-H2029 Growth Inhibition Assay IC50=15.3602 μM SANGER
NCI-H2009 Growth Inhibition Assay IC50=15.5095 μM SANGER
LK-2 Growth Inhibition Assay IC50=15.6449 μM SANGER
NCI-H661 Growth Inhibition Assay IC50=15.9075 μM SANGER
GT3TKB Growth Inhibition Assay IC50=16.0676 μM SANGER
GP5d Growth Inhibition Assay IC50=16.342 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=16.4485 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=16.565 μM SANGER
NB7 Growth Inhibition Assay IC50=16.6971 μM SANGER
NCI-H460 Growth Inhibition Assay IC50=16.7326 μM SANGER
8305C Growth Inhibition Assay IC50=16.7877 μM SANGER
CaR-1 Growth Inhibition Assay IC50=16.8111 μM SANGER
D-247MG Growth Inhibition Assay IC50=16.8625 μM SANGER
LoVo Growth Inhibition Assay IC50=16.9488 μM SANGER
NCI-H2405 Growth Inhibition Assay IC50=17.1908 μM SANGER
AU565 Growth Inhibition Assay IC50=17.225 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=17.5317 μM SANGER
22RV1 Growth Inhibition Assay IC50=17.5884 μM SANGER
HT-144 Growth Inhibition Assay IC50=17.6598 μM SANGER
HuO9 Growth Inhibition Assay IC50=17.7031 μM SANGER
Daoy Growth Inhibition Assay IC50=17.7184 μM SANGER
SJRH30 Growth Inhibition Assay IC50=17.8489 μM SANGER
CHL-1 Growth Inhibition Assay IC50=17.9249 μM SANGER
J82 Growth Inhibition Assay IC50=17.9635 μM SANGER
COR-L23 Growth Inhibition Assay IC50=18.0011 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=18.2276 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=18.4615 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=18.5697 μM SANGER
ES3 Growth Inhibition Assay IC50=18.5883 μM SANGER
MDA-MB-231 Growth Inhibition Assay IC50=18.6502 μM SANGER
MN-60 Growth Inhibition Assay IC50=19.0592 μM SANGER
EPLC-272H Growth Inhibition Assay IC50=19.3708 μM SANGER
SW948 Growth Inhibition Assay IC50=19.3934 μM SANGER
MOLT-13 Growth Inhibition Assay IC50=19.4546 μM SANGER
HL-60 Growth Inhibition Assay IC50=20.2141 μM SANGER
CP50-MEL-B Growth Inhibition Assay IC50=20.4748 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=20.4978 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=20.7967 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=20.906 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=20.9285 μM SANGER
NB12 Growth Inhibition Assay IC50=21.0394 μM SANGER
KY821 Growth Inhibition Assay IC50=21.582 μM SANGER
PSN1 Growth Inhibition Assay IC50=21.6453 μM SANGER
EGI-1 Growth Inhibition Assay IC50=21.7454 μM SANGER
CTV-1 Growth Inhibition Assay IC50=22.3031 μM SANGER
TI-73 Growth Inhibition Assay IC50=22.3498 μM SANGER
LCLC-103H Growth Inhibition Assay IC50=22.4752 μM SANGER
D-542MG Growth Inhibition Assay IC50=22.5558 μM SANGER
ATN-1 Growth Inhibition Assay IC50=22.6439 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=22.8368 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=23.1478 μM SANGER
UM-UC-3 Growth Inhibition Assay IC50=23.1944 μM SANGER
NCI-H1573 Growth Inhibition Assay IC50=23.4681 μM SANGER
NCI-H520 Growth Inhibition Assay IC50=23.4948 μM SANGER
ESS-1 Growth Inhibition Assay IC50=23.8059 μM SANGER
COR-L88 Growth Inhibition Assay IC50=23.9475 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=24.0312 μM SANGER
HCC1937 Growth Inhibition Assay IC50=24.1 μM SANGER
RS4-11 Growth Inhibition Assay IC50=24.142 μM SANGER
HCC38 Growth Inhibition Assay IC50=24.2394 μM SANGER
RPMI-2650 Growth Inhibition Assay IC50=24.6162 μM SANGER
P12-ICHIKAWA Growth Inhibition Assay IC50=24.6258 μM SANGER
YAPC Growth Inhibition Assay IC50=24.8214 μM SANGER
NB13 Growth Inhibition Assay IC50=25.2611 μM SANGER
SK-N-AS Growth Inhibition Assay IC50=25.8584 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=26.049 μM SANGER
LS-411N Growth Inhibition Assay IC50=26.2038 μM SANGER
NCI-H810 Growth Inhibition Assay IC50=26.3112 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=26.5454 μM SANGER
HH Growth Inhibition Assay IC50=26.5529 μM SANGER
U-2-OS Growth Inhibition Assay IC50=26.7382 μM SANGER
SF539 Growth Inhibition Assay IC50=26.8018 μM SANGER
NCI-H2052 Growth Inhibition Assay IC50=27.086 μM SANGER
A673 Growth Inhibition Assay IC50=27.2102 μM SANGER
WM-115 Growth Inhibition Assay IC50=27.7767 μM SANGER
SW48 Growth Inhibition Assay IC50=27.8005 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=27.8532 μM SANGER
PC-3 Growth Inhibition Assay IC50=27.8941 μM SANGER
UMC-11 Growth Inhibition Assay IC50=27.9343 μM SANGER
U-118-MG Growth Inhibition Assay IC50=28.0123 μM SANGER
NCI-H2452 Growth Inhibition Assay IC50=28.0822 μM SANGER
CAMA-1 Growth Inhibition Assay IC50=28.8564 μM SANGER
MC-IXC Growth Inhibition Assay IC50=29.2366 μM SANGER
ES4 Growth Inhibition Assay IC50=29.3172 μM SANGER
BHT-101 Growth Inhibition Assay IC50=29.321 μM SANGER
KP-4 Growth Inhibition Assay IC50=29.516 μM SANGER
CAL-54 Growth Inhibition Assay IC50=29.5445 μM SANGER
5637 Growth Inhibition Assay IC50=29.6421 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=29.7269 μM SANGER
Ca-Ski Growth Inhibition Assay IC50=29.946 μM SANGER
AsPC-1 Growth Inhibition Assay IC50=30.0212 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=30.15 μM SANGER
L-428 Growth Inhibition Assay IC50=30.405 μM SANGER
SW1463 Growth Inhibition Assay IC50=30.5383 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=30.5574 μM SANGER
CAKI-1 Growth Inhibition Assay IC50=30.7702 μM SANGER
YKG-1 Growth Inhibition Assay IC50=31.0263 μM SANGER
A2058 Growth Inhibition Assay IC50=31.1164 μM SANGER
A375 Growth Inhibition Assay IC50=31.1696 μM SANGER
SNB75 Growth Inhibition Assay IC50=31.2435 μM SANGER
SK-HEP-1 Growth Inhibition Assay IC50=31.4271 μM SANGER
ME-180 Growth Inhibition Assay IC50=31.6542 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=31.8247 μM SANGER
HC-1 Growth Inhibition Assay IC50=32.1446 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=32.1971 μM SANGER
SNU-387 Growth Inhibition Assay IC50=32.3191 μM SANGER
C32 Growth Inhibition Assay IC50=32.3353 μM SANGER
EW-13 Growth Inhibition Assay IC50=32.9408 μM SANGER
BFTC-905 Growth Inhibition Assay IC50=33.5136 μM SANGER
NCI-H1299 Growth Inhibition Assay IC50=33.5621 μM SANGER
LU-135 Growth Inhibition Assay IC50=33.801 μM SANGER
NCI-H2122 Growth Inhibition Assay IC50=33.9966 μM SANGER
SK-LMS-1 Growth Inhibition Assay IC50=34.4107 μM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=34.8515 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=35.2747 μM SANGER
MS-1 Growth Inhibition Assay IC50=35.3038 μM SANGER
KYSE-510 Growth Inhibition Assay IC50=35.5042 μM SANGER
NCI-H1793 Growth Inhibition Assay IC50=35.6545 μM SANGER
MIA-PaCa-2 Growth Inhibition Assay IC50=36.0496 μM SANGER
EW-22 Growth Inhibition Assay IC50=36.4072 μM SANGER
IGR-1 Growth Inhibition Assay IC50=36.8184 μM SANGER
HT-1080 Growth Inhibition Assay IC50=37.125 μM SANGER
M14 Growth Inhibition Assay IC50=37.1642 μM SANGER
786-0 Growth Inhibition Assay IC50=37.2794 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=37.4501 μM SANGER
NCI-H510A Growth Inhibition Assay IC50=37.9412 μM SANGER
LAN-6 Growth Inhibition Assay IC50=37.9582 μM SANGER
SW620 Growth Inhibition Assay IC50=38.4974 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=39.8205 μM SANGER
Detroit562 Growth Inhibition Assay IC50=40.1268 μM SANGER
HN Growth Inhibition Assay IC50=40.1782 μM SANGER
HCT-15 Growth Inhibition Assay IC50=40.5907 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=40.9157 μM SANGER
A498 Growth Inhibition Assay IC50=41.3015 μM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=41.4725 μM SANGER
OVCAR-5 Growth Inhibition Assay IC50=41.7767 μM SANGER
NCI-H1792 Growth Inhibition Assay IC50=41.9821 μM SANGER
KOSC-2 Growth Inhibition Assay IC50=42.2699 μM SANGER
Mo-T Growth Inhibition Assay IC50=42.8958 μM SANGER
CFPAC-1 Growth Inhibition Assay IC50=43.4944 μM SANGER
CAL-51 Growth Inhibition Assay IC50=43.5605 μM SANGER
RH-18 Growth Inhibition Assay IC50=43.805 μM SANGER
EC-GI-10 Growth Inhibition Assay IC50=43.8347 μM SANGER
HSC-2 Growth Inhibition Assay IC50=44.009 μM SANGER
ML-2 Growth Inhibition Assay IC50=45.2621 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=45.7365 μM SANGER
NB6 Growth Inhibition Assay IC50=46.111 μM SANGER
MCF7 Growth Inhibition Assay IC50=46.5533 μM SANGER
P30-OHK Growth Inhibition Assay IC50=46.8117 μM SANGER
BPH-1 Growth Inhibition Assay IC50=46.9805 μM SANGER
U251 Growth Inhibition Assay IC50=46.994 μM SANGER
MKN1 Growth Inhibition Assay IC50=47.5137 μM SANGER
A431 Growth Inhibition Assay IC50=47.8338 μM SANGER
C8166 Growth Inhibition Assay IC50=49.2039 μM SANGER
HEL Growth Inhibition Assay IC50=49.4064 μM SANGER
RMG-I Growth Inhibition Assay IC50=49.4444 μM SANGER
CAL-72 Growth Inhibition Assay IC50=49.6075 μM SANGER
SW962 Growth Inhibition Assay IC50=49.9332 μM SANGER
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
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生物活性

产品描述 Axitinib是一种多靶点抑制剂,作用于 VEGFR1VEGFR2VEGFR3,PDGFRβ和c-Kit,在猪主动脉内皮细胞中IC50分别为0.1 nM,0.2 nM,0.1-0.3 nM,1.6 nM和1.7 nM。
特性 Axitinib与目前使用的sorafenib相比,作为二代治疗法,更有效。
靶点
VEGFR1/FLT1 [1]
(Porcine aorta endothelial cells)
VEGFR2/Flk1 [1]
(Porcine aorta endothelial cells)
VEGFR2/KDR [1]
(Porcine aorta endothelial cells)
VEGFR3 [1]
(Porcine aorta endothelial cells)
PDGFRβ [1]
(Porcine aorta endothelial cells)
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0.1 nM 0.18 nM 0.2 nM 0.1 nM-0.3 nM 1.6 nM
体外研究(In Vitro)
体外研究活性 Axitinib是受体激酶抑制剂,作用于VEGFR-1, VEGFR-2,VEGFR-3, PDGFR-β和c-KIT时IC50分别为0.1 , 0.2, 0.1-0.3, 1.6 和1.7 nM 。[1]Axitinib可以阻断VEGFR的自磷酸化作用,VEGF调节的内皮细胞活力,微管形成,及下游信号。Axitinib抑制多种细胞系的增殖,如作用于IGR-N91, IGR-NB8, SH-SY5Y ,无VEGF刺激的HUVEC时IC50分别为>1000 nM, 849 nM, 274 nM和573 nM。[2]
激酶实验 细胞受体激酶磷酸化实验
生成过量表达全长VEGFR-2, PDGFR-β, 和KIT的PAE 细胞,及过量表达鼠VEGFR-2 (Flk-1) 或 PDGFR-α的NIH-3T3细胞。用2.5 µg/mL VEGFR-2抗体, 0.75 µg/mL anti-PDGFR-β 抗体, 0.25 µg/mL anti-PDGFR-α 抗体, 及0.5 µg/mL anti-KIT 抗体包被96孔板,每孔100ul。或者用1.20 µg/mL Flk-1抗体制成酶联免疫吸附(ELISA)捕获板。通过ELISA测定RTK的磷酸化作用。
细胞实验 细胞系 HUVEC,SH-SY5Y, IGR-N91,和IGR-NB8细胞
浓度 1 nM 到10 µM
孵育时间 72小时
方法 HUVEC, SH-SY5Y, IGR-N91和IGR-NB8细胞系按5x104密度接种在96孔板上,培养24小时。加入浓度不等(1 nM到10 µM)的Axitinib。72小时后,通过 MTS四唑基底物测定细胞活力,计算IC50值。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-c-kit / c-kit / p-AKT / AKT / p-ERK / ERK / p-STAT3 / STAT3 / p-STAT5 / STAT5 / p-S6K / S6K / p-S6 / S6 PARP / cleaved PARP / caspase-3 / cleaved caspase-3 31205508
Immunofluorescence alpha-tubulin 26474283
Growth inhibition assay Cell viability 26474283
体内研究(In Vivo)
体内研究活性 Axitinib抑制常位移植模型,如M24met (黑色素瘤), HCT-116 (结肠直肠癌), 和SN12C (肾细胞癌)。[1]活体研究显示,按动物体重,每千克口服处理30mg Axitinib,与没有Axitinib处理的对照组相比,实验组推迟肿瘤生长达到11.4天;且用于IGR-N91侧腹移植瘤时,与对照组(密度为49)相比实验组(密度降为21)降低血管密度。[2]Axitinib在多种肿瘤包括肾细胞癌,甲状腺癌,非小细胞肺癌,黑色素瘤中显示出单一药效活性。
动物实验 Animal Models BT474胸腺癌细胞皮下移植到雌性免疫缺陷小鼠内(Nu/nu;8-12周大)
Dosages 10, 30或100 mg/kg
Administration 每天口服处理
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06161558 Not yet recruiting
Neoplasms
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
May 15 2024 Phase 1
NCT05949632 Recruiting
Advanced Solid Tumors
Incyte Corporation
April 16 2024 Phase 1|Phase 2
NCT05969496 Recruiting
Renal Cancer|Kidney Cancer|Renal Cell Carcinoma|Inferior Vena Cava Thrombosis
University of Colorado Denver|Cancer League of Colorado
December 4 2023 Phase 2
NCT05904730 Enrolling by invitation
Breast Cancer|Ovarian Cancer|Breast Neoplasms|Ovarian Neoplasms|BRCA Mutation|HER2-positive Breast Cancer|HER2-negative Breast Cancer|HER-2 Protein Overexpression
Lynkcell Europe
July 11 2023 Phase 1
NCT05817903 Recruiting
Metastatic Renal Cell Carcinoma
Consorzio Oncotech|Pfizer
April 18 2023 Phase 2
NCT05263609 Withdrawn
Renal Cell Cancer
University of Oklahoma|Merck Sharp & Dohme LLC|Pfizer
June 2022 Phase 2

化学信息&溶解度

分子量 386.47 分子式

C22H18N4OS

CAS号 319460-85-0 SDF Download Axitinib SDF
Smiles CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)C=CC4=CC=CC=N4
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 26 mg/mL ( (67.27 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

体内溶解度
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

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

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)

mg/kg g μL

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,: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: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: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。

技术支持

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操作手册

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常见问题及建议解决方法

问题 1:
We would like to store at -80℃ after it dissolved in CMC. Do you have any infomation about the suggested concentration in CMC?

回答:
Axitinib in 0.5% CMC at up to 30mg/ml is a suspension for oral gavage administration only. We don't suggest customer to freeze down the solution but to make fresh if possible. Customer can store it for 1-2 weeks at 4 degree for continuous use.

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