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首页-小分子抑制剂&激动剂-Tyrosine Kinase-c-Met (HGFR)-SAR 125844
SAR 125844

Chemical Structure : SAR 125844

CAS No.: 1116743-46-4

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SAR 125844 (SAR125844;SAR-125844)

货号: PC-60463Not For Human Use, Lab Use Only.

SAR 125844 is a potent, highly selective, ATP-competitive MET receptor tyrosine kinase inhibitor with IC50 of 4.2 nM.

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1 mg (Free Sample) ￥180 In stock
5 mg ￥780 In stock
10 mg ￥1280 In stock
25 mg ￥2180 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SAR 125844 is a potent, highly selective, ATP-competitive MET receptor tyrosine kinase inhibitor with IC50 of 4.2 nM.
SAR 125844 also inhibits H1094Y, Y1235D, M1250T, L1195V, and D1228H mutants with IC50 of 0.22, 1.7, 6.5, 65, and 81 nM, respectively.
SAR 125844 displays >100-fold selectivity over RON, and good selectivity in a panel of 275 human kinases.
SAR 125844 inhibits phosphorylation of wild-type MET, M1250T, Y1235D, and L1195V MET mutants with IC50 of 8.8, 30, 179, and 591 nM, respectively.
selectively inhibits proliferation in cells with MET gene amplification, promotes apoptosis and inhibits HGF-mediated tumor cell migration; displays potent antitumor activity in vivo models.

物理化学性质&存储条件

分子量 550.631
分子式 C25H23FN8O2S2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1-{6-[6-(4-Fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylsulfanyl]benzothiazol-2-yl}-3-(2-morpholin-4-ylethyl)urea

参考文献

1. Egile C, et al. Mol Cancer Ther. 2015 Feb;14(2):384-94.

2. Ugolini A, et al. J Med Chem. 2016 Aug 11;59(15):7066-74.

3. Shitara K, et al. Oncotarget. 2017 Jun 16;8(45):79546-79555.

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