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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-BBO-10203
BBO-10203

Chemical Structure : BBO-10203

CAS No.: 2971769-60-3

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BBO-10203 (BBO 10203)

货号: PC-24644Not For Human Use, Lab Use Only.

BBO-10203 is a first-in-class inhibitor of the RAS-PI3Kα interaction, binds specifically and cocalently to the RBD of PI3Kα (IC50=3 nM), disrupts PI3Kα interaction with K-,H-, and N-RAS with low single digit nanomolar potency (5 nM).

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

    生物&药学活性

    BBO-10203 is a first-in-class inhibitor of the RAS-PI3Kα interaction, binds specifically and cocalently to the RBD of PI3Kα (IC50=3 nM), disrupts PI3Kα interaction with K-,H-, and N-RAS with low single digit nanomolar potency (5 nM).
    BBO-10203 does not inhibit the kinase activity of PI3Kα, forms covalent bond with C242.
    blocks binding of K-, H-, and N-RAS to PI3Kα.
    BBO-10203 potently inhibits pAKT with single digit nM potency (IC50=4 nM), inhibits basal pAKT cellular levels (BT-474/KYSE-410 IC50: ~5 nM) in HER2 amplified (HER2amp) and wild-type or mutant PI3Ka cell lines.
    BBO-1020 (1-100 mg/kg, PO) induces dependent inhibition of pAKT in KYSE-410 (HER2amp/KRASG12C) tumor bearing mice.
    BBO-10203 daily oral dosing of 30 mg/kg results in significant tumor regressions in KYSE-410 xenograft model.
    BBO-10203 inhibits pAKT leading to monotherapy and combination benefit with KRASi in KRAS mutant tumors.

    物理化学性质&存储条件

    分子量 640.71
    分子式 C34H30F2N6O3S
    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-(2-(7-(2,4-difluoro-6-(2-methoxyethoxy)phenyl)-4-(1-methyl-1H-indazol-5-yl)thieno[3,2-c]pyridin-6-yl)-4-methyl-6,7-dihydropyrazolo[1,5-a]pyrazin-5(4H)-yl)prop-2-en-1-one

    参考文献

    1. Pedro Beltran, et al. Cancer Res (2024) 84 (9_Supplement): RF02-02.

    2. Patent WO2023154282 A1

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