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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-FAPL-PI3Ki1
FAPL-PI3Ki1

Chemical Structure : FAPL-PI3Ki1

CAS No.: 2723568-72-5

FAPL-PI3Ki1

货号: PC-72075Not For Human Use, Lab Use Only.

FAPL-PI3Ki1 is a specific FAP-targeted PI3K inhibitor that selectively targets FAP-expressing human IPF lung fibroblasts and potently inhibits collagen synthesis.

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

    生物&药学活性

    FAPL-PI3Ki1 is a specific FAP-targeted PI3K inhibitor that selectively targets FAP-expressing human IPF lung fibroblasts and potently inhibits collagen synthesis.
    FAPL-PI3Ki1 significantly inhibited phosphorylation of Akt in IPF fibroblasts with IC50 of 200 nM, also inhibited phosphorylation of 4E-BP1.
    FAPL-PI3Ki1 induced suppression of TGFb1-stimulated collagen production and phosphorylation of Akt in IPF fibroblasts requires participation of FAP.
    FAPL-PI3Ki1 suppressed production of hydroxyproline (major building block of collagen), reduced collagen deposition, and increased mouse survival in a mouse model of IPF inhibited PI3K activation in fibrotic lungs.

    物理化学性质&存储条件

    分子量 1177.188
    分子式 C52H48F4N10O12S3
    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

    N-(4-(((4-(((S)-1-((S)-2-cyano-4,4-difluoropyrrolidin-1-yl)-1-oxopropan-2-yl)carbamoyl)pyridin-2-yl)methyl)amino)-4-oxobutanoyl)-S-((2-((((5-(6-(5-((2,4-difluorophenyl)sulfonamido)-6-methoxypyridin-2-yl)quinolin-4-yl)pyridin-2-yl)methoxy)carbonyl)oxy)ethyl)thio)cysteine

    参考文献

    1. Suraj U Hettiarachchi, et al. Sci Transl Med. 2020 Oct 28;12(567):eaay3724.

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