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QR-6401

Chemical Structure : QR-6401

CAS No.: 2845096-18-4

QR-6401 (QR6401)

Catalog No.: PC-20284Not For Human Use, Lab Use Only.

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

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    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

    Physicochemical Properties

    M.Wt 369.43
    Formula C19H23N5O3
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    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

    References

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

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