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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Indoleamine 2,3-Dioxygenase (IDO)-LY3410738
LY3410738

Chemical Structure : LY3410738

CAS No.: 2230263-60-0

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LY3410738 (LY 3410738)

货号: PC-49659Not For Human Use, Lab Use Only.

LY3410738 (LY 3410738) is a potent, selective, and covalent inhibitor of mutant IDH1 (IDH1-R132), LY3410738 is more effective than Ivosidenib (Cat#PC-45550) and potentiates antileukemic activity of AML.

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

    生物&药学活性

    LY3410738 (LY 3410738) is a potent, selective, and covalent inhibitor of mutant IDH1 (IDH1-R132), LY3410738 is more effective than Ivosidenib (Cat#PC-45550) and potentiates antileukemic activity of AML.
    LY3410738 modifies a single cysteine (Cys269) in an allosteric binding pocket and rapidly inactivates the enzyme, selectively inhibiting 2-HG production without affecting alpha-ketoglutarate (a-KG) levels.
    LY3410738 displayed greater potency for inhibition of 2-HG production and differentiation of the IDH1 mutant cells compared to AG-120.
    LY3410738 treatement caused sustained 2-HG inhibition leading to a more robust and durable efficacy with respect to AG-120 in vivo.
    LY3410738 increased efficacy with Cytarabine and Azacitidine or the FLT3 inhibitor Midostaurin, exhibited a potent anti-leukemic effect, reduction of 2-HG level, and enhanced differentiation of the leukemic blasts in FLT3-mutated AML mice.
    LY3410738 also showed synergistic effect when combined with FDA approved Bcl-2 inhibitor, venetoclax in isogenic cells with IDH1R132H mutation, as well as in AML xenograft model derived from a patient refractory to AG-120.

    物理化学性质&存储条件

    分子量 504.64
    分子式 C28H36N6O3
    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

    7-(((S)-1-(4-((S)-1-(4-acryloylpiperazin-1-yl)-2-cyclopropylethyl)phenyl)ethyl)amino)-1-ethyl-1,4-dihydro-2H-pyrimido[4,5-d][1,3]oxazin-2-one

    参考文献

    1. Abstract 6417: Cancer Res (2020) 80 (16_Supplement): 6417.

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