AMG-458 |CAS:913376-83-7 Probechem Biochemicals

Chemical Structure : AMG-458

CAS No.: 913376-83-7

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AMG-458 (AMG458;AMG 458)

货号: PC-36035Not For Human Use, Lab Use Only.

AMG-458 (AMG458) is a potent, selective, orally bioavailable c-Met inhibitor with Ki of 1.2 nM (human c-Met).

规格	价格	库存
5 mg	￥1980	In stock
10 mg	￥2980	In stock
25 mg	￥4880	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

AMG-458 (AMG458) is a potent, selective, orally bioavailable c-Met inhibitor with Ki of 1.2 nM (human c-Met).
AMG-458 also potently binds to mutant c-Met (H1094R), c-Met (V1092I) and c-Met (D1228H) with Ki values of 0.5-2.2 nM.
AMG-458 inhibits HGF-mediated c-Met phosphorylation in PC3 and CT26 cells with IC50 of 60 and 120 nM, abrogates the constitutive phosphorylation of c-Met in H441 cells.
AMG-458 significantly inhibits tumor growth in the NIH3T3/TPR-Met and U-87 MG xenograft models.

物理化学性质&存储条件

分子量	539.592
分子式	C30H29N5O5
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-(2-Hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide

参考文献

1. Liu L, et al. J Med Chem. 2008 Jul 10;51(13):3688-91.

2. Tiedt R, et al. Cancer Res. 2011 Aug 1;71(15):5255-64.

3. van den Heuvel CNAM, et al. Mol Cancer Res. 2017 Nov;15(11):1587-1597.

AMG-458 (AMG458;AMG 458)

生物&药学活性

物理化学性质&存储条件

参考文献

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AMG-458 (AMG458;AMG 458)

生物&药学活性

物理化学性质&存储条件

参考文献

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