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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-AMXI-5001 hydrochloride
AMXI-5001 hydrochloride

Chemical Structure : AMXI-5001 hydrochloride

CAS No.: 2923879-23-4

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AMXI-5001 hydrochloride (AMXI 5001 hydrochloride)

货号: PC-72150Not For Human Use, Lab Use Only.

AMXI-5001 hydrochloride (AMXI 5001) is a novel, highly potent, orally active dual PARP1/2 (IC50 5/0.05 nM) and microtubule polymerization inhibitor, inhibits intracellular PAR formation with IC50 of 7 nM.

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

    生物&药学活性

    AMXI-5001 hydrochloride (AMXI 5001) is a novel, highly potent, orally active dual PARP1/2 (IC50 5/0.05 nM) and microtubule polymerization inhibitor, inhibits intracellular PAR formation with IC50 of 7 nM.
    AMXI-5001 binds to the catalytic domain of human PARP1 and is a weak tankyrase inhibitor (800-fold lower than IC50 towards either PARP1 or PARP2 enzymes).
    AMXI-5001 inhibited tubulin polymerization in a dose-dependent manner.
    AMXI-5001 exhibited selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors.
    AMXI-5001 is highly active in both BRCA mutated and wild type cancers.
    AMXI-5001 elicited a remarkable In vivo preclinical anti-tumor activity in a BRCA mutated TNBC model induced complete regression of established tumors, including exceedingly large tumors, demonstrated superior anti-tumor effects compared to either single agent (PARP or microtubule) inhibitor or combination with both agents.

    物理化学性质&存储条件

    分子量 493.923
    分子式 C25H21ClFN5O3
    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

    ethyl (6-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)phenyl)-1H-benzo[d]imidazol-2-yl)carbamate hydrochloride

    参考文献

    1. Hassan Lemjabbar-Alaoui, et al. Am J Cancer Res. 2020 Aug 1;10(8):2649-2676.

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