MK-8353 hydrochloride |CAS:1951448-73-9 Probechem Biochemicals

Chemical Structure : MK-8353 hydrochloride

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MK-8353 hydrochloride (MK8353)

货号: PC-62596Not For Human Use, Lab Use Only.

MK-8353 hydrochloride (SCH-900353) is a highly potent, orally bioavailable, dual-specificity ERK1/2 inhibitor with IC50 of 23.0/8.8 nM, respectively.

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生物&药学活性

MK-8353 hydrochloride (SCH-900353) is a highly potent, orally bioavailable, dual-specificity ERK1/2 inhibitor with IC50 of 23.0/8.8 nM, respectively; inhibits nonactivated ERK2 with IC50 of 0.5 nM, demonstrates excellent kinase selectivity over a 227-human kinase panel; decreases pERK1, pERK2, and ribosomal S6 kinase (pRSK) proteins, with complete suppression of pERK1 and pERK2 observed at 30 nM in A2058 cells, inhibits the in vitro proliferation of a panel of BRAFV600-mutant and RAS-mutant cancer cell lines; exhibits in vivo antitumor activity against BRAFV600 mutant Colo-205 colon cancer model and the BRAFV600 mutant SK-MEL-28 melanoma model.

Colon Cancer

Phase 1 Clinical

物理化学性质&存储条件

分子量	728.313
分子式	C37H42ClN9O3S
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	(S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide hydrochloride

参考文献

1. Moschos SJ, et al. JCI Insight. 2018 Feb 22;3(4). pii: 92352.

MK-8353 hydrochloride (MK8353)

生物&药学活性

物理化学性质&存储条件

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MK-8353 hydrochloride (MK8353)

生物&药学活性

物理化学性质&存储条件

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