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ASTX660 hydrochloride

Chemical Structure : ASTX660 hydrochloride

CAS No.: 1799328-50-9

ASTX660 hydrochloride (Tolinapant, ASTX-660)

货号: PC-63392Not For Human Use, Lab Use Only.

Tolinapant (ASTX660) hydrochloride is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM.

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

    生物&药学活性

    Tolinapant (ASTX660) hydrochloride is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM.
    Tolinapant (ASTX660) potently inhibits association between XIAP and caspase 9 in HEK293 cell line with EC50 of 2.8 nM, binds to and leads to the degradation of cIAP1/2 and stabilisation of NIK in cells.
    Tolinapant (ASTX660) induces apoptosis in MDA-MB-231 cells with EC50 of 1.8 nM, which is TNF-α-dependent; inhibits tumor growth in mice bearing breast and melanoma tumor xenografts.

    物理化学性质&存储条件

    分子量 612.612
    分子式 C30H44Cl2FN5O3
    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

    1-(6-(4-fluorobenzyl)-5-(hydroxymethyl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)-2-((2R,5R)-5-methyl-2-(((R)-3-methylmorpholino)methyl)piperazin-1-yl)ethan-1-one dihydrochloride

    参考文献

    1. Ward GA, et al. Mol Cancer Ther. 2018 Apr 25. pii: molcanther.0848.2017.

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