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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-ERK-MK-8353 hydrochloride
MK-8353 hydrochloride

Chemical Structure : MK-8353 hydrochloride

CAS No.: 1951448-73-9

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MK-8353 hydrochloride (MK8353, SCH 900353)

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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    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.
    MK-8353 inhibits nonactivated ERK2 with IC50 of 0.5 nM.
    MK-8353 demonstrates excellent kinase selectivity over a 227-human kinase panel.
    MK-8353 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.
    MK-8353 exhibits in vivo antitumor activity against BRAFV600 mutant Colo-205 colon cancer model and the BRAFV600 mutant SK-MEL-28 melanoma model.

    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.

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