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首页-小分子抑制剂&激动剂-Cytoskeleton/Cell Adhesion Molecules-Kinesin-AM-9022
AM-9022

Chemical Structure : AM-9022

CAS No.: 2446872-46-2

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AM-9022 (AM9022)

货号: PC-21658Not For Human Use, Lab Use Only.

AM-9022 (AM9022) is a potent, selective and orally active mitotic kinesin KIF18A inhibitor with IC50 of 47 nM in kinesin-8 microtubule (MT)-ATPase motor assays.

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

    生物&药学活性

    AM-9022 (AM9022) is a potent, selective and orally active mitotic kinesin KIF18A inhibitor with IC50 of 47 nM in kinesin-8 microtubule (MT)-ATPase motor assays.
    AM-9022 exhibits good specificity against a panel of diverse kinesin motor proteins, except for the KIF19A motor (IC50=926 nM).
    AM-9022 shows cellular EC50 of 42 and 37 nM for cell line pH3+ and PCM foci in mitotic image assays respectively.
    AM-9022 has similar inhibitory effects on the motor activity of human and mouse KIF18A.
    AM-9022 (30 mg per kg, p.o.) increased pH3 mitotic marker levels in OVCAR-3 tumors by 3.4-fold in the OVCAR-3 HGSOC CDX tumor model, inhibited tumor growth with evidence of TR (95% TR) and no body weight loss.
    AM-9022 administered at 30 and 100 mg per kg inhibited tumor growth with evidence of TR (16% and 94% TR, respectively) at well-tolerated doses in JIMT-1 breast cancer CDX tumor model.

    物理化学性质&存储条件

    分子量 578.68
    分子式 C27H36F2N6O4S
    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

    (R)-N-(2-(4,4-difluoropiperidin-1-yl)-6-methylpyrimidin-4-yl)-4-((2-hydroxy-1-methylethyl)sulfonamido)-2-(6-azaspiro[2.5]octan-6-yl)benzamide

    参考文献

    1. Marc Payton, et al. Nat Cancer. 2023 Dec 27. doi: 10.1038/s43018-023-00699-5.

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