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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-PF-06862309
PF-06862309

Chemical Structure : PF-06862309

CAS No.: 2067281-52-9

PF-06862309 (PF-06843195 phosphate ester prodrug)

货号: PC-49022Not For Human Use, Lab Use Only.

PF-06862309 (PF-06843195 phosphate ester prodrug) is the in vivo-active, phosphate ester prodrug of PF-06843195, a potent selective PI3Kα inhibitor with Kd of <18 pM.

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

    生物&药学活性

    PF-06862309 (PF-06843195 phosphate ester prodrug) is the in vivo-active, phosphate ester prodrug of PF-06843195, a potent selective PI3Kα inhibitor with Kd of <18 pM.
    PF-06862309 demonstrated robust PK/PD correlation and tumor growth inhibition (TGI) in mouse xenograft models with MDAMB361 and MCF7 cell lines.
    PF-06862309 is a clinical candidate for treating breast cancer patients characterized with ER+ , HER2-, and harboring PIK3CA mutations.

    物理化学性质&存储条件

    分子量 578.446
    分子式 C20H26F3N8O7P
    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

    2,2-difluoroethyl (S)-3-((2'-amino-5-fluoro-2-morpholino-[4,5'-bipyrimidin]-6-yl)amino)-3-((phosphonooxy)methyl)pyrrolidine-1-carboxylate

    参考文献

    1. Cheng H, et al. J Med Chem. 2021 Jan 14;64(1):644-661.

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