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SY-5102

Chemical Structure : SY-5102

CAS No.: 2365230-48-2

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SY-5102 (SY5102)

Catalog No.: PC-72466Not For Human Use, Lab Use Only.

SY-5102 (SY5102) is a highly potent, selective, noncovalent, orally available CDK7 inhibitor with SPR Kd of 0.03 nM (binding to CDK7/Cyclin H).

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

    Biological Activity

    SY-5102 (SY5102) is a highly potent, selective, noncovalent, orally available CDK7 inhibitor with SPR Kd of 0.03 nM (binding to CDK7/Cyclin H).
    SY-5102 (SY5102) displays highly selectivity against CDK2, CDK9, and CDK12 (all IC50>75 nM).
    SY-5102 potently inhibits HCC70 cell proliferation with EC50 of 9 nM.
    SY-5102 showed dose-dependent tumor growth inhibition including tumor regression at 4 mg/kg po (dosed twice daily) in an HCC70 cell line derived xenograft mouse model.

    Physicochemical Properties

    M.Wt 457.45
    Formula C22H22F3N7O
    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

    (S)-4-(6-(3,5-Dimethylisoxazol-4-yl)-1H-pyrrolo[2,3-b]pyridin-3-yl)-N-(piperidin-3-yl)-5-(trifluoromethyl)pyrimidin-2-amine hydrochloride

    References

    1. Jason J Marineau, et al. J Med Chem. 2022 Jan 27;65(2):1458-1480.

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