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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MEK (MAP2K)-DS03090629
DS03090629

Chemical Structure : DS03090629

CAS No.:

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DS03090629 (DS 03090629)

货号: PC-49634Not For Human Use, Lab Use Only.

DS03090629 is a potent, selective, ATP-competitive and orally available MEK1/2 inhibitor, shows high affinity for the MEK protein regardless of its phosphorylation status (npMEK (inactive) Kd=0.11 nM, and pMEK (active) Kd=0.15 nM).

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

    生物&药学活性

    DS03090629 is a potent, selective, ATP-competitive and orally available MEK1/2 inhibitor, shows high affinity for the MEK protein regardless of its phosphorylation status (npMEK (inactive) Kd=0.11 nM, and pMEK (active) Kd=0.15 nM).
    DS03090629 is effective for BRAF-overexpressing melanoma cell lines (A375_mock, IC50=37.1 nM; A375_BRAF, IC50=74.3 nM).
    DS03090629 exhibits tendencies to retain inhibitory activities against both WT MEK1 and F53L mutant against wild-type pMEK1 and mutated pMEK1 in a cell-free enzymatic assays.
    DS03090629 is effective against not only BRAF-overexpressing cancers, but also MEK1-mutated cancer cells.
    DS03090629 also exhibits superior efficacy against a melanoma cell line expressing mutant MEK1 protein compared with dabrafenib and trametinib.
    DS03090629 (75 mg/kg, mpk, QD) combined with dabrafenib significantly inhibited ERK phosphorylation, induced tumor regression in the A375_mock or A375_BRAF xenograft models.

    物理化学性质&存储条件

    分子量 463.97
    分子式 C25H26ClN5O2
    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

    (1R,3S)-3-((6-(2-chloro-4-((4-methylpyrimidin-2-yl)oxy)phenyl)-3-methyl-1H-indazol-4-yl)oxy)cyclohexan-1-amine

    参考文献

    1. Kohei Takano, et al. Mol Cancer Ther. 2023 Jan 9;MCT-22-0306.

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