Dasatinib

别名: BMS-354825 中文名称：达沙替尼

目录号：S1021 Purity: 99.95%

Dasatinib是一种新型有效的多靶点抑制剂，作用于Abl、Src和 c-Kit，在无细胞试验中IC50分别为 <1 nM、0.8 nM 和 79 nM。Dasatinib 可诱导自噬和凋亡并具有抗肿瘤的活性。

Dasatinib Chemical Structure

CAS: 302962-49-8

规格	价格	库存
10mM (1mL in DMSO)	794.43	现货
25mg	647.01	现货
100mg	1556.1	现货
500mg	3349.71	现货
1g	5487.3	现货
更大包装有超大折扣
400-668-6834 info@selleck.cn

产品质控

批次： S102108 DMSO]98 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false 纯度： 99.95%

99.95

常与Dasatinib一起在实验中被使用的化合物

Olaparib (AZD2281)

Dasatinib和Olaparib联合可诱导细胞周期阻滞，并以caspase依赖的方式诱导MDA-MB-231/HS-578T细胞凋亡。

Fisetin

在动物模型中，Dasatinib和Fisetin诱导衰老细胞凋亡，产生健康益处，并延长寿命。

Quercetin

Dasatinib和Quercetin治疗可延缓肠道细胞衰老，减轻炎症负担，并调节老年小鼠的肠道菌群。

Imatinib

与Imatinib相比，Dasatinib在费城染色体阳性急性淋巴细胞白血病(ALL)治疗中显示出优越的结果。

Nilotinib

Dasatinib和Nilotinib是酪氨酸激酶抑制剂(TKIs)，用于费城染色体阳性慢性髓性白血病(CML)的一线治疗。

Dasatinib相关产品

相关靶点	Lck Fyn Lyn Yes Fgr	点击展开
相关产品	Saracatinib (AZD0530) PP2 SU6656 PP1 WH-4-023 Src Inhibitor 1 Tolimidone (MLR-1023) UM-164 Myristic Acid RK 24466 eCF506	点击展开
相关化合物库	酪氨酸激酶抑制剂分子库 PI3K/Akt 抑制剂库血管生成相关化合物库 HIF-1信号通路化合物库 FDA抗癌药物库	点击展开

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(PMID)
MDA-MB-231	Antitumor assay	40 mg/kg/day	18 days	Antitumor activity against human MDA-MB-231 cells xenografted in SCID mouse assessed as tumor growth inhibition at 40 mg/kg/day administered for 18 days measured every 3 days during compound dosing	25835317
MDA-MB-231	Antiproliferative assay	>0.01 uM	12 days	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of colony formation at >0.01 uM after 12 days by crystal violet staining-based assay	25835317
MDA-MB-231	Function assay	0.001 to 1 uM	20 hrs	Inhibition of Src phosphorylation in human MDA-MB-231 cells at 0.001 to 1 uM after 20 hrs by Western blot analysis	25835317
MDA-MB-231	Antimigratory assay	0.03 to 0.3 uM	20 hrs	Antimigratory activity against human MDA-MB-231 cells at 0.03 to 0.3 uM after 20 hrs by wound healing assay	25835317
MDA-MB-231	Function assay	>0.03 uM	20 hrs	Inhibition of Src in human MDA-MB-231 cells assessed as reduction of FAK phosphorylation at >0.03 uM after 20 hrs by Western blot analysis	25835317
MDA-MB-231	Cell cycle assay	0.3 uM	24 to 48 hrs	Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G0/G1 phase at 0.3 uM after 24 to 48 hrs by flow cytometric analysis	25835317
MDA-MB-231	Antiinvasive assay	0.1 uM	24 hrs	Antiinvasive activity against human MDA-MB-231 cells at 0.1 uM after 24 hrs by transwell assay	25835317
SH-SY5Y	Apoptosis assay	0.1 uM	24 hrs	Induction of apoptosis in human SH-SY5Y cells assessed as accumulation of hypodiploid cells at 0.1 uM after 24 hrs by propidium iodide staining-based cytofluorimetry	25469771
murine mast cell	Function Assay	1 μM	24 h	Inhibits antigen-induced IL6 secretion in IgE primed mouse mast cells at 1 uM	17684099
U937	Function Assay	1 μM	1 h	Reduces LPS-induced TNFalpha release in human U937 cells	17684099
U937	Function Assay	1 μM	1 h	Reduces basal TNFalpha release in human U937 cells	17684099
C6/36	Antiviral Assay	2.5 μM	4 days	Inhibits viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM	17360676
Huh7	Antiviral Assay	2.5 μM	4 days	Inhibits viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM	17360676
DU145	Kinase Assay	0.1 μM	5 h	Inhibits cSrc in human DU145 cells assessed as reduction of phosphorylated FAK Y576/Y577 level at 100 nM	19462975
PC3	Kinase Assay	0.1 μM	5 h	Inhibits cSrc in human PC3 cells assessed as reduction of phosphorylated FAK Y576/Y577 level at 100 nM	19462975
DU145	Kinase Assay	0.1 μM	5 h	Inhibits cSrc in human DU145 cells assessed as reduction of phosphorylated Src Y416 level at 100 nM	19462975
PC3	Kinase Assay	0.1 μM	5 h	Inhibits cSrc in human PC3 cells assessed as reduction of phosphorylated Src Y416 level at 100 nM	19462975
DU145	Function Assay	0.1 μM	5 h	Inhibits human DU145 cell adhesion at 100 nM	19462975
PC3	Function Assay	0.1 μM	5 h	Inhibits human PC3 cell adhesion at 100 nM	19462975
Plasmodium falciparum	Function Assay	10 μM	15 min	Inhibits Plasmodium falciparum proliferation by inhibiting the Function of PfCDPK1 protein with IC50 of 1.17μM	24550330
HUVEC	Function Assay	15 μM	72 h	Induces antiangiogenic activity in HUVEC co-cultured with vascular smooth muscle cells assessed as Inhibition of network formation at 1.8 to 15 uM	22853993
HUVEC	Growth Inhibition Assay	0.15 μM	72 h	Induces antiangiogenic activity in HUVEC co-cultured with vascular smooth muscle cells assessed as Inhibition of cell growth at 0.15 uM	22853993
ALL3	Cytotoxic Assay	0.1μM	72 h	IC50=0.0004 μM	19889540
KU812	Function assay	0.1 uM	1 hr	Inhibition of BCR/ABL in human KU812 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method	26789553
KU812	Function assay	0.1 uM	1 hr	Inhibition of BCR/ABL in human KU812 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method	26789553
MEG01	Function assay	0.1 uM	1 hr	Inhibition of BCR/ABL in human MEG01 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method	26789553
MEG01	Function assay	0.1 uM	1 hr	Inhibition of BCR/ABL in human MEG01 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method	26789553
K562	Function assay	0.1 uM	1 hr	Inhibition of BCR/ABL in human K562 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method	26789553
K562	Function assay	0.1 uM	1 hr	Inhibition of BCR/ABL in human K562 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method	26789553
MDA-MB-231	Function assay	3 to 100 nM	1.5 hrs	Inhibition of SRC phosphorylation at tyrosine 416 in human MDA-MB-231 cells at 3 to 100 nM preincubated for 1.5 hrs followed by serum stimulation for 1 hr by Western blot analysis	27115835
MDA-MB-231	Function assay	3 to 100 nM	1.5 hrs	Inhibition of FAK phosphorylation at tyrosine 861 in human MDA-MB-231 cells at 3 to 100 nM preincubated for 1.5 hrs followed by serum stimulation for 1 hr by Western blot analysis	27115835
MDA-MB-231	Antimigratory assay	10 nM	6 hrs	Antimigratory activity in human MDA-MB-231 cells assessed as reduction in cell motility at 10 nM at 6 hrs by microscopy based scratch-wound cell migration assay	27115835
MCF7	Antiproliferative assay	0.03 to 300 uM	5 days	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability at 0.03 to 300 uM after 5 days by PrestoBlue assay	27115835
B16-BL6	Function assay	8.13 uM	24 to 48 hrs	Inhibition of cell migration of mouse B16-BL6 cells at 8.13 uM incubated for 24 to 48 hrs by cell wound scratch assay	29395973
MCF7	Function assay	7.5 uM	10 days	Inhibition of colony formation in human MCF7 cells at 7.5 uM incubated for 10 days by crystal violet staining based plate cloning test	29395973
HEK293	Function Assay	10 μM		Induces binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells with IC50 of 0.063μM	22770610
BA/F3	Function assay		72 hrs	GI50 = 0.004 μM	26789553
BA/F3	Function assay		72 hrs	GI50 = 0.003 μM	26789553
BA/F3	Function assay		72 hrs	GI50 = 0.003 μM	26789553
BA/F3	Function assay		72 hrs	GI50 = 0.003 μM	26789553
BA/F3	Function assay		72 hrs	GI50 = 0.003 μM	26789553
BA/F3	Function assay		72 hrs	GI50 = 0.001 μM	26789553
BA/F3	Function assay		72 hrs	GI50 = 0.001 μM	26789553
BA/F3	Function assay		72 hrs	GI50 = 0.001 μM	26789553
MEG01	Antiproliferative assay		72 hrs	GI50 = 0.0003 μM	26789553
KU812	Antiproliferative assay		72 hrs	GI50 = 0.0003 μM	26789553
BA/F3	Function assay		72 hrs	GI50 = 0.0003 μM	26789553
K562	Cytotoxicity assay		48 hrs	IC50 = 0.45 μM	26451772
K562	Antiproliferative assay		72 hrs	GI50 = 0.0003 μM	26789553
K562	Antiproliferative assay		72 hrs	IC50 = 0.001 μM	26195136
NCI-H2286	Antiproliferative assay		72 hrs	IC50 = 0.032 μM	26191369
HCC366	Antiproliferative assay		72 hrs	IC50 = 0.029 μM	26191369
MCF7	Cytotoxicity assay		48 hrs	IC50 = 8.05 μM	25899332
MDA-MB-231	Cytotoxicity assay		48 hrs	IC50 = 1.12 μM	25899332
MDA-MB-231	Cytotoxicity assay		72 hrs	IC50 = 0.178 μM	25835317
HEK293	Cytotoxicity assay		72 hrs	IC50 = 14.3 μM	25815152
A2780	Cytotoxicity assay		72 hrs	IC50 = 8.7 μM	25815152
ECRF24	Cytotoxicity assay		72 hrs	IC50 = 5.7 μM	25815152
CXF 1103L	Antiproliferative assay		4 days	GI50 = 4.36 μM	25076195
GXF251L	Antiproliferative assay		4 days	GI50 = 2.25 μM	25076195
PRXF DU145	Antiproliferative assay		4 days	GI50 = 0.0623 μM	25076195
PAXF 1657L	Antiproliferative assay		4 days	GI50 = 0.121 μM	25076195
LXFA 983L	Antiproliferative assay		4 days	GI50 = 0.0565 μM	25076195
RXF 393NL	Antiproliferative assay		4 days	GI50 = 0.0217 μM	25076195
Sf9	Function assay		20 mins	IC50 = 27.3 μM	23956101
Sf9	Function assay		15 to 20 mins	IC50 = 13.1 μM	23956101
Ba/F3	Function assay		1 hr	Inhibition of Bcr-Abl T315I mutant (unknown origin) phosphorylation transfected in mouse Ba/F3 cells after 1 hr by Western blot analysis	23600806
Ba/F3	Function assay		1 hr	Inhibition of Bcr-Abl T315I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction of phosphorylated CrkL level after 1 hr by Western blot analysis	23600806
Ba/F3	Function assay		1 hr	Inhibition of Bcr-Abl T315I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction of phosphorylated STAT5 level after 1 hr by Western blot analysis	23600806
Sf21	Function assay		5 mins	IC50 = 10 μM	22961681
U937	Cytotoxicity assay		72 hrs	IC50 = 13.63 μM	22217877
K562	Cytotoxicity assay		72 hrs	IC50 = 12.83 μM	22217877
FDC-P1	Function assay		48 hrs	IC50 = 0.0074 μM	20156689
U937	Growth Inhibition Assay		72 h	IC50=12.2 μM	23567960
A549	Growth Inhibition Assay		72 h	IC50=8.2 μM	23567960
NCI-H661	Growth Inhibition Assay		72 h	IC50=7.8 μM	23567960
DLD1	Growth Inhibition Assay		72 h	IC50=4.6 μM	23567960
NCI-H460	Growth Inhibition Assay		72 h	IC50=8.99 μM	23521020
MCF7	Growth Inhibition Assay		72 h	IC50=2.57 μM	23521020
HCT116	Growth Inhibition Assay		72 h	IC50=2.3 μM	23521020
NCI-H23	Growth Inhibition Assay		72 h	IC50=2.27 μM	23521020
GXF251L	Cytotoxic Assay		4 days	IC50=2.25 μM	23253074
CXF 1103L	Cytotoxic Assay		4 days	IC50=4.36 μM	23253074
PAXF 1657L	Cytotoxic Assay		4 days	IC50=0.121 μM	23253074
PRXF DU145	Cytotoxic Assay		4 days	IC50=0.0623 μM	23253074
LXFA 983L	Cytotoxic Assay		4 days	IC50=0.0565 μM	23253074
RXF 393NL	Cytotoxic Assay		4 days	IC50=0.0217 μM	23253074
SW620	Cytotoxic Assay		72 h	GI50=8.43 μM	24015327
KM12	Cytotoxic Assay		72 h	GI50=7.44 μM	24015327
MALME-3M	Cytotoxic Assay		72 h	GI50=6.61 μM	24015327
NCI60	Cytotoxic Assay		72 h	GI50=5.7 μM	24015327
U251	Cytotoxic Assay		72 h	GI50=2.81 μM	24015327
DU145	Cytotoxic Assay		72 h	GI50=0.16 μM	24015327
HMEC	Cytotoxic Assay		72 h	GI50=1.8 μM	24015327
Hs578T	Cytotoxic Assay		72 h	GI50=0.03 μM	24015327
MDA-MB-231	Growth Inhibition Assay		72 h	IC50=0.012 μM	15615512
PC3	Growth Inhibition Assay		72 h	IC50=0.0094 μM	15615512
WiDr	Growth Inhibition Assay		72 h	IC50=0.052 μM	15615512
T cell	Growth Inhibition Assay		72 h	Inhibits anti CD3- and anti CD28-induced T cell proliferation with IC50 of 0.003μM	17154512
BA/F3	Growth Inhibition Assay		72 h	Induces cytotoxicity against mouse BA/F3 cells assessed as growth Inhibition with IC50 of 2.5μM	23301703
BA/F3	Growth Inhibition Assay		72 h	Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth Inhibition with IC50 of 3.6μM	23301703
BA/F3	Growth Inhibition Assay		72 h	Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth Inhibition with IC50 of 0.0023μM	23301703
BA/F3	Growth Inhibition Assay		72 h	Induces cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth Inhibition with IC50 of 0.0019μM	23301703
BA/F3	Growth Inhibition Assay		72 h	Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth Inhibition with IC50 of 0.0013μM	23301703
BA/F3	Growth Inhibition Assay		72 h	Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth Inhibition with IC50 of 0.008μM	23301703
BA/F3	Growth Inhibition Assay		72 h	Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth Inhibition with IC50 of 0.0051μM	23301703
BA/F3	Growth Inhibition Assay		72 h	Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth Inhibition with IC50 of 0.0032μM	23301703
BA/F3	Growth Inhibition Assay		72 h	Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth Inhibition with IC50 of 0.0009μM	23301703
BA/F3	Growth Inhibition Assay		72 h	Induces antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant with IC50 of 1.714μM	23088644
BA/F3	Growth Inhibition Assay		72 h	Induces antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl with IC50 of 0.0045μM	23088644
BA/F3	Growth Inhibition Assay		72 h	Induces antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant with IC50 of 0.00083μM	23088644
BA/F3	Growth Inhibition Assay		72 h	IC50=6.589 μM	23088644
CML	Growth Inhibition Assay		20 min	IC50=0.001 μM	19219016
M07e	Growth Inhibition Assay		72 h	IC50=0.0012 μM	17956080
K562	Growth Inhibition Assay		72 h	IC50=0.001 μM	17956080
M07ep210	Growth Inhibition Assay		72 h	IC50=0.00007 μM	17956080
BA/F3	Function assay		72 hrs	GI50 = 0.004 μM	26789553
BA/F3	Function assay		72 hrs	GI50 = 0.005 μM	26789553
BA/F3	Function assay		72 hrs	GI50 = 0.008 μM	26789553
BA/F3	Function assay		72 hrs	GI50 = 0.008 μM	26789553
BA/F3	Function assay		72 hrs	GI50 = 0.01 μM	26789553
BA/F3	Function assay		72 hrs	GI50 = 0.014 μM	26789553
BA/F3	Function assay		72 hrs	GI50 = 0.014 μM	26789553
BA/F3	Function assay		72 hrs	GI50 = 0.017 μM	26789553
BA/F3	Function assay		72 hrs	GI50 = 0.039 μM	26789553
CHL	Antiproliferative assay		72 hrs	GI50 = 0.27 μM	26789553
MOLM14	Antiproliferative assay		72 hrs	GI50 = 2.3 μM	26789553
BA/F3	Function assay		72 hrs	GI50 = 3 μM	26789553
BA/F3	Function assay		72 hrs	GI50 = 3 μM	26789553
MV4-11	Antiproliferative assay		72 hrs	GI50 = 3.6 μM	26789553
HEL	Antiproliferative assay		72 hrs	GI50 = 5.3 μM	26789553
BA/F3	Function assay		72 hrs	GI50 = 9.94 μM	26789553
K562	Cytotoxicity assay		72 hrs	IC50 = 0.00025 μM	26814890
BA/F3	Cytotoxicity assay		72 hrs	IC50 = 0.09 μM	26814890
BAF3	Function assay		72 hrs	EC50 = 0.00004 μM	27010810
BAF3	Function assay		72 hrs	EC50 = 0.00004 μM	27010810
BxPC3	Antiproliferative assay		72 hrs	EC50 = 0.033 μM	27010810
MDA-MB-231	Antiproliferative assay		72 hrs	EC50 = 0.044 μM	27010810
Caki2	Antiproliferative assay		72 hrs	EC50 = 0.055 μM	27010810
NCI-H1975	Antiproliferative assay		72 hrs	EC50 = 0.173 μM	27010810
PC3	Antiproliferative assay		72 hrs	EC50 = 0.232 μM	27010810
insect	Function assay		20 mins	IC50 = 0.0005 μM	27115835
MDA-MB-231	Antiproliferative assay		5 days	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 5 days by PrestoBlue assay	27115835
HCT116	Cytotoxicity assay		96 hrs	IC50 = 5.23 μM	27155464
A549	Cytotoxicity assay		96 hrs	IC50 = 8.37 μM	27155464
U937	Cytotoxicity assay		96 hrs	IC50 = 10.23 μM	27155464
K562	Cytotoxicity assay		96 hrs	IC50 = 11.95 μM	27155464
HEK293	Function assay		1 hr	Ki = 0.0005 μM	29941193
HEK293	Function assay		1 hr	IC50 = 0.006 μM	29941193
Ba/F3	Function assay		48 hrs	GI50 = 0.00021 μM	30137981
Ba/F3	Function assay		48 hrs	GI50 = 0.00025 μM	30137981
Ba/F3	Function assay		48 hrs	GI50 = 0.00029 μM	30137981
Ba/F3	Function assay		48 hrs	GI50 = 0.0003 μM	30137981
Ba/F3	Function assay		48 hrs	GI50 = 0.00033 μM	30137981
Ba/F3	Function assay		48 hrs	GI50 = 0.00042 μM	30137981
Ba/F3	Function assay		48 hrs	GI50 = 0.00077 μM	30137981
Ba/F3	Function assay		48 hrs	GI50 = 0.00098 μM	30137981
Ba/F3	Function assay		48 hrs	GI50 = 0.00144 μM	30137981
Ba/F3	Function assay		48 hrs	GI50 = 2.562 μM	30137981
HEK293	Cytotoxicity assay			CC50 = 16 μM	26264503
THP1	Cytotoxicity assay			IC50 = 6 μM	26264503
K562	Cytotoxicity assay			IC50 = 0.08 μM	26264503
IR-K562	Cytotoxicity assay			IC50 = 1.9 μM	26264503
HMC-1.2	Antiproliferative assay			IC50 = 0.82 μM	25004409
K562	Cytotoxicity assay			CC50 = 0.25 μM	27474918
K562	Antiproliferative assay			GI50 = 0.001 μM	28435526
K562	Function assay			IC50 = 0.000069 μM	29395973
HL60	Function assay			IC50 = 0.00011 μM	29395973
KG1a	Function assay			IC50 = 8.98 μM	29395973
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) 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
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 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
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Vero	qHTS assay			Vero cells viability qHTS for Zika virus inhibitors	33229545
HepG2	qHTS assay			HepG2 cells viability qHTS for Zika virus inhibitors	33229545
BV-173	Growth Inhibition Assay			IC50=0.000000109 μM	SANGER
K-562	Growth Inhibition Assay			IC50=0.000000266 μM	SANGER
BL-70	Growth Inhibition Assay			IC50=0.000000822 μM	SANGER
EM-2	Growth Inhibition Assay			IC50=0.00000108 μM	SANGER
LAMA-84	Growth Inhibition Assay			IC50=0.00000321 μM	SANGER
MEG-01	Growth Inhibition Assay			IC50=0.0000098 μM	SANGER
EoL-1-cell	Growth Inhibition Assay			IC50=0.0000131 μM	SANGER
CTV-1	Growth Inhibition Assay			IC50=0.0000404 μM	SANGER
TE-15	Growth Inhibition Assay			IC50=0.00589 μM	SANGER
NOS-1	Growth Inhibition Assay			IC50=0.00613 μM	SANGER
D-336MG	Growth Inhibition Assay			IC50=0.0063 μM	SANGER
LB1047-RCC	Growth Inhibition Assay			IC50=0.00989 μM	SANGER
LB996-RCC	Growth Inhibition Assay			IC50=0.00991 μM	SANGER
SW982	Growth Inhibition Assay			IC50=0.01115 μM	SANGER
TK10	Growth Inhibition Assay			IC50=0.01174 μM	SANGER
A704	Growth Inhibition Assay			IC50=0.01491 μM	SANGER
TE-8	Growth Inhibition Assay			IC50=0.01576 μM	SANGER
DOHH-2	Growth Inhibition Assay			IC50=0.01719 μM	SANGER
HOP-62	Growth Inhibition Assay			IC50=0.01834 μM	SANGER
TE-12	Growth Inhibition Assay			IC50=0.01861 μM	SANGER
KGN	Growth Inhibition Assay			IC50=0.01942 μM	SANGER
NCI-H1648	Growth Inhibition Assay			IC50=0.02011 μM	SANGER
OS-RC-2	Growth Inhibition Assay			IC50=0.0203 μM	SANGER
GB-1	Growth Inhibition Assay			IC50=0.02157 μM	SANGER
RXF393	Growth Inhibition Assay			IC50=0.02357 μM	SANGER
LC-2-ad	Growth Inhibition Assay			IC50=0.02586 μM	SANGER
KS-1	Growth Inhibition Assay			IC50=0.0273 μM	SANGER
ETK-1	Growth Inhibition Assay			IC50=0.02832 μM	SANGER
SW954	Growth Inhibition Assay			IC50=0.02927 μM	SANGER
Becker	Growth Inhibition Assay			IC50=0.03003 μM	SANGER
MZ1-PC	Growth Inhibition Assay			IC50=0.03119 μM	SANGER
ES6	Growth Inhibition Assay			IC50=0.03193 μM	SANGER
KURAMOCHI	Growth Inhibition Assay			IC50=0.03487 μM	SANGER
CGTH-W-1	Growth Inhibition Assay			IC50=0.03548 μM	SANGER
VA-ES-BJ	Growth Inhibition Assay			IC50=0.03902 μM	SANGER
LXF-289	Growth Inhibition Assay			IC50=0.03956 μM	SANGER
MPP-89	Growth Inhibition Assay			IC50=0.04049 μM	SANGER
SW872	Growth Inhibition Assay			IC50=0.04161 μM	SANGER
SNB75	Growth Inhibition Assay			IC50=0.04435 μM	SANGER
PSN1	Growth Inhibition Assay			IC50=0.04474 μM	SANGER
LB831-BLC	Growth Inhibition Assay			IC50=0.04609 μM	SANGER
MFH-ino	Growth Inhibition Assay			IC50=0.04724 μM	SANGER
TGBC24TKB	Growth Inhibition Assay			IC50=0.04761 μM	SANGER
A388	Growth Inhibition Assay			IC50=0.05095 μM	SANGER
BB30-HNC	Growth Inhibition Assay			IC50=0.05437 μM	SANGER
GI-ME-N	Growth Inhibition Assay			IC50=0.06118 μM	SANGER
TGBC1TKB	Growth Inhibition Assay			IC50=0.06164 μM	SANGER
TE-10	Growth Inhibition Assay			IC50=0.06357 μM	SANGER
A498	Growth Inhibition Assay			IC50=0.07284 μM	SANGER
TE-11	Growth Inhibition Assay			IC50=0.07858 μM	SANGER
BB65-RCC	Growth Inhibition Assay			IC50=0.08227 μM	SANGER
C2BBe1	Growth Inhibition Assay			IC50=0.08308 μM	SANGER
NCI-H747	Growth Inhibition Assay			IC50=0.08362 μM	SANGER
IST-MES1	Growth Inhibition Assay			IC50=0.08552 μM	SANGER
KALS-1	Growth Inhibition Assay			IC50=0.0949 μM	SANGER
GCIY	Growth Inhibition Assay			IC50=0.09656 μM	SANGER
RL95-2	Growth Inhibition Assay			IC50=0.1038 μM	SANGER
TE-1	Growth Inhibition Assay			IC50=0.1054 μM	SANGER
NCI-H1355	Growth Inhibition Assay			IC50=0.11028 μM	SANGER
SW962	Growth Inhibition Assay			IC50=0.11292 μM	SANGER
KLE	Growth Inhibition Assay			IC50=0.11317 μM	SANGER
MC116	Growth Inhibition Assay			IC50=0.1141 μM	SANGER
NMC-G1	Growth Inhibition Assay			IC50=0.11606 μM	SANGER
KU812	Growth Inhibition Assay			IC50=0.11883 μM	SANGER
COLO-829	Growth Inhibition Assay			IC50=0.12213 μM	SANGER
NTERA-S-cl-D1	Growth Inhibition Assay			IC50=0.12283 μM	SANGER
IST-MEL1	Growth Inhibition Assay			IC50=0.1345 μM	SANGER
MLMA	Growth Inhibition Assay			IC50=0.14032 μM	SANGER
LS-123	Growth Inhibition Assay			IC50=0.14064 μM	SANGER
LB2518-MEL	Growth Inhibition Assay			IC50=0.14162 μM	SANGER
NB69	Growth Inhibition Assay			IC50=0.14436 μM	SANGER
8-MG-BA	Growth Inhibition Assay			IC50=0.15458 μM	SANGER
K5	Growth Inhibition Assay			IC50=0.16489 μM	SANGER
KINGS-1	Growth Inhibition Assay			IC50=0.16666 μM	SANGER
SF268	Growth Inhibition Assay			IC50=0.17404 μM	SANGER
PF-382	Growth Inhibition Assay			IC50=0.17678 μM	SANGER
SH-4	Growth Inhibition Assay			IC50=0.18413 μM	SANGER
NALM-6	Growth Inhibition Assay			IC50=0.19295 μM	SANGER
CP66-MEL	Growth Inhibition Assay			IC50=0.19531 μM	SANGER
697	Growth Inhibition Assay			IC50=0.19987 μM	SANGER
CP67-MEL	Growth Inhibition Assay			IC50=0.20488 μM	SANGER
DSH1	Growth Inhibition Assay			IC50=0.24001 μM	SANGER
HCE-4	Growth Inhibition Assay			IC50=0.26439 μM	SANGER
MZ2-MEL	Growth Inhibition Assay			IC50=0.28537 μM	SANGER
BL-41	Growth Inhibition Assay			IC50=0.29123 μM	SANGER
HUTU-80	Growth Inhibition Assay			IC50=0.3142 μM	SANGER
LOXIMVI	Growth Inhibition Assay			IC50=0.31503 μM	SANGER
no-10	Growth Inhibition Assay			IC50=0.31931 μM	SANGER
KARPAS-422	Growth Inhibition Assay			IC50=0.33997 μM	SANGER
SW684	Growth Inhibition Assay			IC50=0.3498 μM	SANGER
SF126	Growth Inhibition Assay			IC50=0.3541 μM	SANGER
D-263MG	Growth Inhibition Assay			IC50=0.36224 μM	SANGER
OVCAR-4	Growth Inhibition Assay			IC50=0.37433 μM	SANGER
BB49-HNC	Growth Inhibition Assay			IC50=0.38599 μM	SANGER
ONS-76	Growth Inhibition Assay			IC50=0.42951 μM	SANGER
MZ7-mel	Growth Inhibition Assay			IC50=0.47911 μM	SANGER
RCC10RGB	Growth Inhibition Assay			IC50=0.4911 μM	SANGER
BOKU	Growth Inhibition Assay			IC50=0.49133 μM	SANGER
no-11	Growth Inhibition Assay			IC50=0.50228 μM	SANGER
IST-SL2	Growth Inhibition Assay			IC50=0.50302 μM	SANGER
RKO	Growth Inhibition Assay			IC50=0.52966 μM	SANGER
HT-144	Growth Inhibition Assay			IC50=0.53609 μM	SANGER
NCI-H446	Growth Inhibition Assay			IC50=0.6276 μM	SANGER
QIMR-WIL	Growth Inhibition Assay			IC50=0.70629 μM	SANGER
MHH-PREB-1	Growth Inhibition Assay			IC50=0.74469 μM	SANGER
EW-16	Growth Inhibition Assay			IC50=0.76178 μM	SANGER
EW-24	Growth Inhibition Assay			IC50=0.78165 μM	SANGER
LB373-MEL-D	Growth Inhibition Assay			IC50=0.82508 μM	SANGER
TE-9	Growth Inhibition Assay			IC50=0.87532 μM	SANGER
A3-KAW	Growth Inhibition Assay			IC50=0.98452 μM	SANGER
A101D	Growth Inhibition Assay			IC50=1.03043 μM	SANGER
OCUB-M	Growth Inhibition Assay			IC50=1.04412 μM	SANGER
ES4	Growth Inhibition Assay			IC50=1.05145 μM	SANGER
TE-6	Growth Inhibition Assay			IC50=1.21226 μM	SANGER
D-502MG	Growth Inhibition Assay			IC50=1.23376 μM	SANGER
KNS-42	Growth Inhibition Assay			IC50=1.24412 μM	SANGER
SNU-C2B	Growth Inhibition Assay			IC50=1.30589 μM	SANGER
NCI-H1838	Growth Inhibition Assay			IC50=1.30733 μM	SANGER
NKM-1	Growth Inhibition Assay			IC50=1.30859 μM	SANGER
GI-1	Growth Inhibition Assay			IC50=1.3622 μM	SANGER
NB5	Growth Inhibition Assay			IC50=1.39827 μM	SANGER
CAS-1	Growth Inhibition Assay			IC50=1.40992 μM	SANGER
HCE-T	Growth Inhibition Assay			IC50=1.56714 μM	SANGER
SBC-1	Growth Inhibition Assay			IC50=1.57984 μM	SANGER
JiyoyeP-2003	Growth Inhibition Assay			IC50=1.73466 μM	SANGER
TE-5	Growth Inhibition Assay			IC50=1.79139 μM	SANGER
CAN	Growth Inhibition Assay			IC50=1.82252 μM	SANGER
SK-UT-1	Growth Inhibition Assay			IC50=2.16693 μM	SANGER
JVM-2	Growth Inhibition Assay			IC50=2.36284 μM	SANGER
LB771-HNC	Growth Inhibition Assay			IC50=2.57551 μM	SANGER
NCCIT	Growth Inhibition Assay			IC50=2.86616 μM	SANGER
NCI-H2126	Growth Inhibition Assay			IC50=2.87552 μM	SANGER
Calu-6	Growth Inhibition Assay			IC50=3.05741 μM	SANGER
SK-LMS-1	Growth Inhibition Assay			IC50=3.11886 μM	SANGER
ARH-77	Growth Inhibition Assay			IC50=3.46915 μM	SANGER
NB17	Growth Inhibition Assay			IC50=3.63847 μM	SANGER
A253	Growth Inhibition Assay			IC50=3.73246 μM	SANGER
OPM-2	Growth Inhibition Assay			IC50=4.27685 μM	SANGER
MV-4-11	Growth Inhibition Assay			IC50=4.36454 μM	SANGER
SR	Growth Inhibition Assay			IC50=4.49954 μM	SANGER
KG-1	Growth Inhibition Assay			IC50=4.60845 μM	SANGER
OCI-AML2	Growth Inhibition Assay			IC50=5.86154 μM	SANGER
D-247MG	Growth Inhibition Assay			IC50=6.12519 μM	SANGER
DJM-1	Growth Inhibition Assay			IC50=6.48558 μM	SANGER
RPMI-6666	Growth Inhibition Assay			IC50=7.27067 μM	SANGER
KARPAS-45	Growth Inhibition Assay			IC50=7.51671 μM	SANGER
LP-1	Growth Inhibition Assay			IC50=7.54782 μM	SANGER
RS4-11	Growth Inhibition Assay			IC50=7.65787 μM	SANGER
DU-4475	Growth Inhibition Assay			IC50=8.21652 μM	SANGER
MONO-MAC-6	Growth Inhibition Assay			IC50=8.27066 μM	SANGER
NCI-SNU-16	Growth Inhibition Assay			IC50=8.56128 μM	SANGER
SJSA-1	Growth Inhibition Assay			IC50=8.72805 μM	SANGER
MMAC-SF	Growth Inhibition Assay			IC50=8.79307 μM	SANGER
SK-NEP-1	Growth Inhibition Assay			IC50=8.89155 μM	SANGER
J-RT3-T3-5	Growth Inhibition Assay			IC50=8.96529 μM	SANGER
SKM-1	Growth Inhibition Assay			IC50=9.01734 μM	SANGER
LB2241-RCC	Growth Inhibition Assay			IC50=9.02012 μM	SANGER
SIG-M5	Growth Inhibition Assay			IC50=9.02493 μM	SANGER
EVSA-T	Growth Inhibition Assay			IC50=9.27793 μM	SANGER
GT3TKB	Growth Inhibition Assay			IC50=9.35546 μM	SANGER
NB6	Growth Inhibition Assay			IC50=9.92259 μM	SANGER
EHEB	Growth Inhibition Assay			IC50=10.0656 μM	SANGER
HEL	Growth Inhibition Assay			IC50=10.4776 μM	SANGER
ALL-PO	Growth Inhibition Assay			IC50=10.7938 μM	SANGER
TGW	Growth Inhibition Assay			IC50=11.2828 μM	SANGER
BC-3	Growth Inhibition Assay			IC50=12.1138 μM	SANGER
IA-LM	Growth Inhibition Assay			IC50=12.4445 μM	SANGER
UACC-257	Growth Inhibition Assay			IC50=12.9198 μM	SANGER
KP-N-YS	Growth Inhibition Assay			IC50=12.9283 μM	SANGER
Raji	Growth Inhibition Assay			IC50=13.7497 μM	SANGER
SF539	Growth Inhibition Assay			IC50=13.8557 μM	SANGER
DMS-153	Growth Inhibition Assay			IC50=14.0028 μM	SANGER
L-540	Growth Inhibition Assay			IC50=15.0672 μM	SANGER
MN-60	Growth Inhibition Assay			IC50=15.1979 μM	SANGER
RPMI-8866	Growth Inhibition Assay			IC50=17.4454 μM	SANGER
NCI-H510A	Growth Inhibition Assay			IC50=19.3973 μM	SANGER
NB13	Growth Inhibition Assay			IC50=19.4877 μM	SANGER
HAL-01	Growth Inhibition Assay			IC50=19.7543 μM	SANGER
NCI-H720	Growth Inhibition Assay			IC50=20.2733 μM	SANGER
REH	Growth Inhibition Assay			IC50=20.6357 μM	SANGER
KNS-81-FD	Growth Inhibition Assay			IC50=23.146 μM	SANGER
HC-1	Growth Inhibition Assay			IC50=24.5551 μM	SANGER
NCI-H2141	Growth Inhibition Assay			IC50=24.7754 μM	SANGER
MOLT-4	Growth Inhibition Assay			IC50=26.6753 μM	SANGER
OMC-1	Growth Inhibition Assay			IC50=27.1422 μM	SANGER
LC-1F	Growth Inhibition Assay			IC50=27.3245 μM	SANGER
NCI-H1304	Growth Inhibition Assay			IC50=28.1628 μM	SANGER
BC-1	Growth Inhibition Assay			IC50=28.651 μM	SANGER
NCI-H64	Growth Inhibition Assay			IC50=29.6253 μM	SANGER
MOLT-16	Growth Inhibition Assay			IC50=29.6292 μM	SANGER
U-87-MG	Growth Inhibition Assay			IC50=30.766 μM	SANGER
GAK	Growth Inhibition Assay			IC50=31.2686 μM	SANGER
ES8	Growth Inhibition Assay			IC50=32.1252 μM	SANGER
HCC1599	Growth Inhibition Assay			IC50=32.3325 μM	SANGER
EB-3	Growth Inhibition Assay			IC50=34.3117 μM	SANGER
HCC1187	Growth Inhibition Assay			IC50=35.8052 μM	SANGER
SK-PN-DW	Growth Inhibition Assay			IC50=36.1943 μM	SANGER
JVM-3	Growth Inhibition Assay			IC50=37.2338 μM	SANGER
HCC2157	Growth Inhibition Assay			IC50=37.9946 μM	SANGER
A4-Fuk	Growth Inhibition Assay			IC50=38.1009 μM	SANGER
COR-L279	Growth Inhibition Assay			IC50=40.2851 μM	SANGER
DEL	Growth Inhibition Assay			IC50=41.9086 μM	SANGER
NCI-H1395	Growth Inhibition Assay			IC50=42.0163 μM	SANGER
MHH-NB-11	Growth Inhibition Assay			IC50=43.0818 μM	SANGER
NCI-H2107	Growth Inhibition Assay			IC50=43.4846 μM	SANGER
NEC8	Growth Inhibition Assay			IC50=44.336 μM	SANGER
COLO-684	Growth Inhibition Assay			IC50=46.2258 μM	SANGER
LS-411N	Growth Inhibition Assay			IC50=48.4748 μM	SANGER
点击查看更多细胞系数据

生物活性

产品描述

靶点

LCK ^[1]	Abl ^[1] (Cell-free assay)	Src ^[1] (Cell-free assay)	c-Kit (D816V) ^[2] (Cell-free assay)	c-Kit (wt) ^[2] (Cell-free assay)
	0.6 nM	0.8 nM	37 nM	79 nM

体外研究(In Vitro)
体外研究活性	在抑制表达野生型Bcr-Abl或全部Bcr-Abl突变型（除了T315I）的Ba/F3增殖时，Dasatinib效果高很多。Dasatinib呈2倍指数增长效力(约325倍)。Dasatinib有效抑制野生型Abl 激酶和全部突变型（除了T315I）。Dasatinib 直接靶向作用于野生型和突变型Abl激酶域，且抑制自磷酸化和底物磷酸化，这种作用存在浓度依赖性。Dasatinib作用于表达野生型 Bcr-Abl的细胞时，效果高325倍多。^[1] TgE骨髓细胞菌落百分数从未处理孔的100% 降低到Dasatinib处理孔的4.12%。有 Dasatinib存在时, WT 和TgE骨髓细胞形成的菌落百分数明显不同。LMP2A的表达可促进 B 淋巴细胞存活和增殖，而Dasatinib通过靶向作用于Lyn 和/或c-Abl 激酶可抑制以上存活和增殖。^[2] Dasatinib 处理一系列甲状腺癌细胞，抑制Src信号, 降低生长速度,使细胞周期停滞，且诱导凋亡。使用剂量不断增加的 Dasatinib (0.019 μM 到 1.25 μM) 处理C643, TPC1, BCPAP, 和 SW1736 细胞3天，抑制50%细胞生长，然而抑制K1细胞系生长则需更高浓度Dasatinib。使用10 nM 或50 nM Dasatinib 处理BCPAP，SW1736 和 K1 细胞，导致G1期细胞提高9-22%，而S期细胞百分数则降低7-18%。^[3]
激酶实验	激酶自磷酸化分析
激酶实验	使用野生型和突变型谷胱甘肽S-转移酶(GST)-Abl融合蛋白 (c-Abl氨基酸220-498位) 进行激酶实验。从谷胱甘肽琼脂糖珠中释放GST-Abl融合蛋白，ATP浓度为5 μM。在用于激酶自磷酸化和体外肽底物磷酸化实验前, 用LAR酪氨酸磷酸酶处理GST-Abl 激酶域融合蛋白。在 30^oC下温育1小时后,加入1 mM 钒酸钠，激活LAR磷酸酶。进行免疫印迹分析，比较未处理的GST-Abl激酶和去磷酸化的GST-Abl激酶，使用磷酸化的特点抗体4G10来确认酪氨酸残基完全去磷酸化(>95%)，使用c-Abl抗体 CST 2862 来确认GST-Abl激酶的平衡负载。实验测定IC50值时所用Dasatinib浓度为0 nM到32 nM。Dasatinib作用于突变型T315I时浓度达到 1,000 nM。在体外肽底物磷酸化实验中使用相同抑制剂浓度。作用于GST-Src激酶和 GST-Lyn激酶的三种抑制剂的浓度范围相同。
细胞实验	细胞系	Ba/F3细胞系
	浓度	0 nM-32 nM
	孵育时间	72小时
	方法	Ba/F3 细胞系重复培养三份，然后与浓度逐渐升高的 Dasatinib 温育72小时。通过MTS活性实验测定细胞增殖。IC50值和IC90值取自三组独立实验的平均值。Dasatinib作用的IC50值和IC90值为0 nM 到32 nM 。Dasatinib 作用于突变型T315I时所需浓度达到200 nM。
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	phospho-c-Abl(Tyr245) / phospho-c-Src(Tyr416) p27 / p21 p-FAK / p-STAT3 cleaved caspase 3		23049975
	Growth inhibition assay	IC50		23721490
	Immunofluorescence	SRC / Met F-actin / Actinin-4 / Paxillin α-tubulin		26517812
	ELISA	TNF-α E-selectin VCAM-1		17684099

体内研究(In Vivo)
体内研究活性	Dasatinib 作用于LMP2A/MYC 双转基因小鼠，可逆转脾肿大。Dasatinib 作用于TgE小鼠抑制表达LMP2A 的骨髓B 细胞形成的菌落，且使脾脏变小。使用Dasatinib处理Tg6/λ-MYC 小鼠，与对照组相比，脾脏质量明显降低。Dasatinib 作用于LMP2A/MYC 双转基因小鼠，抑制淋巴结肿大。Dasatinib作用于嫁接LMP2A/MYC双转基因小鼠肿瘤细胞的Rag1KO小鼠，可逆转脾肿大。Dasatinib 作用于表达LMP2A的B 淋巴细胞瘤，抑制Lyn磷酸化。^[2]
动物实验	Animal Models	EμLMP2A(TgE 和Tg6品种),MYC (λ-MYC), 和LMP2A/λ-MYC双转基因小鼠(Tg6/λ-MYC)
	Dosages	30 mg/kg
	Administration	腹腔注射

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)
NCT05527418	Recruiting	Recent HIV-1 Infection	Eva Bonfill\|Institut d''Investigacions Biomèdiques August Pi i Sunyer	January 26 2024	Phase 2
NCT05993949	Recruiting	Lymphoblastic Leukemia	Stanford University\|Kite Pharma	October 2 2023	Phase 1
NCT05780073	Recruiting	HIV Infection Primary	Fundació Institut Germans Trias i Pujol\|Fundación FLS de Lucha Contra el Sida Enfermedades Infecciosas y Promoción de la Salud y Ciencia\|Spanish Clinical Research Network - SCReN\|IrsiCaixa\|University of Turin Italy\|Instituto de Salud Carlos III\|Germans Trias i Pujol Hospital	October 16 2023	Phase 2
NCT05198843	Terminated	Anatomic Stage IV Breast Cancer AJCC v8\|Metastatic Triple-Negative Breast Inflammatory Carcinoma	National Cancer Institute (NCI)	November 8 2022	Phase 1\|Phase 2
NCT04925648	Recruiting	Metastatic Prostate Cancer	St Vincent''s Hospital Sydney	October 18 2021	Phase 2

参考文献
https://pubmed.ncbi.nlm.nih.gov/15930265/ https://pubmed.ncbi.nlm.nih.gov/16434489/ https://pubmed.ncbi.nlm.nih.gov/22609829/ https://pubmed.ncbi.nlm.nih.gov/22586301/ + 展开

参考文献

https://pubmed.ncbi.nlm.nih.gov/15930265/
https://pubmed.ncbi.nlm.nih.gov/16434489/
https://pubmed.ncbi.nlm.nih.gov/22609829/

https://pubmed.ncbi.nlm.nih.gov/22586301/

+ 展开

化学信息&溶解度

分子量	488.01	分子式	C₂₂H₂₆ClN₇O₂S
CAS号	302962-49-8	SDF	Download Dasatinib SDF
Smiles	CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=CC(=NC(=N3)C)N4CCN(CC4)CCO
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 : 98 mg/mL ( (200.81 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

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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常见问题及建议解决方法

问题 1:
what’s the difference between S1021 and S7782? Which one is better for in vivo studies?

回答：
Usually, hydrate will be more stable and dissolve better than free base. But this compound (S1021) dissolves better in DMSO than hydrate one (S7782).

问题 2:
Can I give dasatinib to mice by oral gavage? If so, how to dissolve the drug?

回答：
Our S1021 Dasatinib in 1% DMSO+30% PEG 300+1% Tween 80 at 30 mg/ml is a suspension which you can administrate to mice via oral gavage. If you want a clear solution, it can be dissolved in 4% DMSO+30% PEG 300+5% Tween 80+ddH2O at 5 mg/ml clearly.

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):