SAR125844 is a potent and highly selective c-Met inhibitor with potential antineoplastic activity. Upon intravenous administration, SAR125844 binds to c-Met, thereby disrupting c-Met-mediated signal transduction pathways. SAR125844 displayed nanomolar activity against the wild-type kinase (IC50 value of 4.2 nmol/L) and the M1250T and Y1235D mutants. Broad biochemical profiling revealed that SAR125844 was highly selective for MET kinase. SAR125844 inhibits MET autophosphorylation in cell-based assays in the nanomolar range, and promotes low nanomolar proapoptotic and antiproliferative activities selectively in cell lines with MET gene amplification or pathway addiction.
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化学信息
名称 | SAR125844 |
Iupac 化学名称 | 1-(6-((6-(4-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)thio)benzo[d]thiazol-2-yl)-3-(2-morpholinoethyl)urea |
同义词 | SAR125844 |
英文同义词 | SAR125844 |
分子式 | C25H23FN8O2S2 |
分子量 | 550.6314 |
Smile | FC1=CC=C(C=C1)C=1C=CC=2N(N1)C(=NN2)SC2=CC1=C(N=C(S1)NC(=O)NCCN1CCOCC1)C=C2 |
InChiKey | ODIUNTQOXRXOIV-UHFFFAOYSA-N |
InChi | InChI=1S/C25H23FN8O2S2/c26-17-3-1-16(2-4-17)19-7-8-22-30-31-25(34(22)32-19)37-18-5-6-20-21(15-18)38-24(28-20)29-23(35)27-9-10-33-11-13-36-14-12-33/h1-8,15H,9-14H2,(H2,27,28,29,35) |
Cas号 | 1116743-46-4 |
相关CAS号 | |
外观性状 | Solid powder |
纯度 | 98% by HPLC |
存储 | -20 ºC for 3 years |
可溶性 | Soluble in DMSO |
处理方式 | |
运输条件 | Shipped under ambient temperature |
海关编码 | |
Targets | |
Mechanism | |
Cell study | |
Animal study | |
Clinical study | |