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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-QR-6401
QR-6401

Chemical Structure : QR-6401

CAS No.: 2845096-18-4

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QR-6401 (QR6401)

货号: PC-20284Not For Human Use, Lab Use Only.

QR-6401 (QR6401) is a highly potent, selective, oral macrocyclic CDK2 inhibitor.

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

    生物&药学活性

    QR-6401 (QR6401) is a highly potent, selective, oral macrocyclic CDK2 inhibitor with IC50 of 0.37 nM (CDK2/Cyclin E1).
    QR-6401 exhibits good selectivity against other closely related kinases, such as CDK1, CDK4, CDK6, CDK9 and GSK3β.
    QR-6401 demonstrates good intrinsic metabolic stability and acceptable plasma protein binding in different species.
    QR-6401 ( twice daily through oral gavage at 50 mg/kg for 28 days) caused significant tumor growth inhibition (TGI% = 78%) in OVCAR3 ovarian cancer xenograft model, produced robust suppression of Rb phosphorylation

    物理化学性质&存储条件

    分子量 369.43
    分子式 C19H23N5O3
    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

    (11S,13R,71R,73S,Z)-21H-6,10-dioxa-3,8-diaza-4(2,6)-pyridina-2(5,3)-pyrazola-1(1,3)-cyclopentana-7(1,3)-cyclobutanacyclodecaphan-9-one

    参考文献

    1. Yang Yu, et al. ACS Med Chem Lett. 2023 Feb 8;14(3):297-304.

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