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Dasatinib

別名: BMS-354825 中文名稱：達(dá)沙替尼

Dasatinib是一種新型有效的多靶點(diǎn)抑制劑，作用于Abl、Src和 c-Kit，在無細(xì)胞試驗(yàn)中IC50分別為 <1 nM、0.8 nM 和 79 nM。Dasatinib 可誘導(dǎo)自噬和凋亡并具有抗腫瘤的活性。

Dasatinib Chemical Structure

Dasatinib Chemical Structure

CAS: 302962-49-8

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mM (1mL in DMSO) 794.43 現(xiàn)貨
25mg 647.01 現(xiàn)貨
100mg 1556.1 現(xiàn)貨
500mg 3349.71 現(xiàn)貨
1g 5487.3 現(xiàn)貨
更大包裝 有超大折扣

400-668-6834

info@selleck.cn
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產(chǎn)品質(zhì)控

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

常與Dasatinib一起在實(shí)驗(yàn)中被使用的化合物

Olaparib (AZD2281)

Dasatinib和Olaparib聯(lián)合可誘導(dǎo)細(xì)胞周期阻滯，并以caspase依賴的方式誘導(dǎo)MDA-MB-231/HS-578T細(xì)胞凋亡。

Corrales-Sanchez V, et al. J Cell Mol Med. 2020 Mar;24(5):3117-3127.

Fisetin

在動(dòng)物模型中，Dasatinib和Fisetin誘導(dǎo)衰老細(xì)胞凋亡，產(chǎn)生健康益處，并延長壽命。

Martel J, et al. Med Res Rev. 2020 Nov;40(6):2114-2131.

Trametinib (GSK1120212)

Dasatinib和Quercetin治療加劇肥胖和年齡依賴性肝病的進(jìn)展。

Blagosklonny MV, et al. Oncotarget. 2021 Aug 31; 12(18): 1821–1835.

Imatinib

與Imatinib相比，Dasatinib在費(fèi)城染色體陽性急性淋巴細(xì)胞白血病(ALL)治療中顯示出優(yōu)越的結(jié)果。

Shen S, et al. JAMA Oncol. 2020 Mar 1;6(3):358-366.

Nilotinib

Dasatinib和Nilotinib是酪氨酸激酶抑制劑(TKIs)，用于費(fèi)城染色體陽性慢性髓性白血病(CML)的一線治療。

Miura M, et al. Biol Pharm Bull. 2015;38(5):645-54.

Dasatinib相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

Src Signaling Pathways

Src信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
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
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述 Dasatinib是一種新型有效的多靶點(diǎn)抑制劑，作用于Abl、Src和 c-Kit，在無細(xì)胞試驗(yàn)中IC50分別為 <1 nM、0.8 nM 和 79 nM。Dasatinib 可誘導(dǎo)自噬和凋亡并具有抗腫瘤的活性。
靶點(diǎn)
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
體外研究(In Vitro)
體外研究活性

在抑制表達(dá)野生型Bcr-Abl或全部Bcr-Abl突變型（除了T315I）的Ba/F3增殖時(shí)，Dasatinib效果高很多。Dasatinib呈2倍指數(shù)增長效力(約325倍)。Dasatinib有效抑制野生型Abl 激酶和全部突變型（除了T315I）。Dasatinib 直接靶向作用于野生型和突變型Abl激酶域，且抑制自磷酸化和底物磷酸化，這種作用存在濃度依賴性。Dasatinib作用于表達(dá)野生型 Bcr-Abl的細(xì)胞時(shí)，效果高325倍多。[1] TgE骨髓細(xì)胞菌落百分?jǐn)?shù)從未處理孔的100% 降低到Dasatinib處理孔的4.12%。 有 Dasatinib存在時(shí), WT 和TgE骨髓細(xì)胞形成的菌落百分?jǐn)?shù)明顯不同。LMP2A的表達(dá)可促進(jìn) B 淋巴細(xì)胞存活和增殖，而Dasatinib通過靶向作用于Lyn 和/或c-Abl 激酶可抑制以上存活和增殖。[2] Dasatinib 處理一系列甲狀腺癌細(xì)胞，抑制Src信號(hào), 降低生長速度,使細(xì)胞周期停滯，且誘導(dǎo)凋亡。使用劑量不斷增加的 Dasatinib (0.019 μM 到 1.25 μM) 處理C643, TPC1, BCPAP, 和 SW1736 細(xì)胞3天，抑制50%細(xì)胞生長，然而抑制K1細(xì)胞系生長則需更高濃度Dasatinib。使用10 nM 或50 nM Dasatinib 處理BCPAP，SW1736 和 K1 細(xì)胞，導(dǎo)致G1期細(xì)胞提高9-22%，而S期細(xì)胞百分?jǐn)?shù)則降低7-18%。[3]
激酶實(shí)驗(yàn) 激酶自磷酸化分析
使用野生型和突變型谷胱甘肽S-轉(zhuǎn)移酶(GST)-Abl融合蛋白 (c-Abl氨基酸220-498位) 進(jìn)行激酶實(shí)驗(yàn)。從谷胱甘肽瓊脂糖珠中釋放GST-Abl融合蛋白，ATP濃度為5 μM。在用于激酶自磷酸化和體外肽底物磷酸化實(shí)驗(yàn)前, 用LAR酪氨酸磷酸酶處理GST-Abl 激酶域融合蛋白。在 30oC下溫育1小時(shí)后,加入1 mM 釩酸鈉，激活LAR磷酸酶。進(jìn)行免疫印跡分析，比較未處理的GST-Abl激酶和去磷酸化的GST-Abl激酶，使用磷酸化的特點(diǎn)抗體4G10來 確認(rèn)酪氨酸殘基完全去磷酸化(>95%)，使用c-Abl抗體 CST 2862 來確認(rèn)GST-Abl激酶的平衡負(fù)載。實(shí)驗(yàn)測(cè)定IC50值時(shí)所用Dasatinib濃度為0 nM到32 nM。Dasatinib作用于突變型T315I時(shí)濃度達(dá)到 1,000 nM。在體外肽底物磷酸化實(shí)驗(yàn)中使用相同抑制劑濃度。作用于GST-Src激酶和 GST-Lyn激酶的三種抑制劑的濃度范圍相同。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 Ba/F3細(xì)胞系
濃度 0 nM-32 nM
孵育時(shí)間 72小時(shí)
方法

Ba/F3 細(xì)胞系重復(fù)培養(yǎng)三份，然后與濃度逐漸升高的 Dasatinib 溫育72小時(shí)。通過MTS活性實(shí)驗(yàn)測(cè)定細(xì)胞增殖。IC50值和IC90值取自三組獨(dú)立實(shí)驗(yàn)的平均值。Dasatinib作用的IC50值和IC90值為0 nM 到32 nM 。Dasatinib 作用于突變型T315I時(shí)所需濃度達(dá)到200 nM。
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 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
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

Dasatinib 作用于LMP2A/MYC 雙轉(zhuǎn)基因小鼠，可逆轉(zhuǎn)脾腫大。Dasatinib 作用于TgE小鼠 抑制表達(dá)LMP2A 的骨髓B 細(xì)胞形成的菌落，且使脾臟變小。使用Dasatinib處理Tg6/λ-MYC 小鼠，與對(duì)照組相比，脾臟質(zhì)量明顯降低。Dasatinib 作用于LMP2A/MYC 雙轉(zhuǎn)基因小鼠，抑制淋巴結(jié)腫大。Dasatinib作用于嫁接LMP2A/MYC雙轉(zhuǎn)基因小鼠腫瘤細(xì)胞的Rag1KO小鼠，可逆轉(zhuǎn)脾腫大。Dasatinib 作用于表達(dá)LMP2A的B 淋巴細(xì)胞瘤，抑制Lyn磷酸化。[2]
動(dòng)物實(shí)驗(yàn) Animal Models EμLMP2A(TgE 和Tg6品種),MYC (λ-MYC), 和LMP2A/λ-MYC雙轉(zhuǎn)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
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

化學(xué)信息&溶解度

分子量 488.01 分子式

C22H26ClN7O2S
CAS號(hào) 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
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 98 mg/mL ( (200.81 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

技術(shù)支持

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常見問題及建議解決方法

問題 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).

問題 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.

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