A Cdk9 inhibitor
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KB-0742 (hydrochloride)

Item No. 39772

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(1S,3S)-N1-[5-(1-ethylpropyl)pyrazolo[1,5-a]pyrimidin-7-yl]-1,3-cyclopentanediamine, monohydrochloride
Molecular Formula
C16H25N5 • HCl
Formula Weight
323.9
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/mlPBS (pH 7.2): Sparingly soluble: 1-10 mg/ml
SMILES
CCC(CC)C1=NC2=CC=NN2C(N[C@@H]3C[C@@H](N)CC3)=C1.Cl
InChi Code
InChI=1S/C16H25N5.ClH/c1-3-11(4-2)14-10-16(19-13-6-5-12(17)9-13)21-15(20-14)7-8-18-21;/h7-8,10-13,19H,3-6,9,17H2,1-2H3;1H/t12-,13-;/m0./s1
InChi Key
FBUAQCCPWMHKGM-QNTKWALQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $105

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    10 mg

    $189

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    25 mg

    $418

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    50 mg

    $732

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    Product Description

    KB-0742 is an inhibitor of cyclin-dependent kinase 9 (Cdk9; IC50 = 6 nM).1 It is selective for Cdk9 over Cdk1-8 (IC50s = 397->10,000 nM) and Cdk12-19 (IC50s = 372->10,000 nM). KB-0742 (0.64-7.73 µM) induces cell cycle arrest at the G1 phase and apoptosis in BT-20, BT-549, MDA-MB-231, MT-3, and Hs 578T triple-negative breast cancer (TNBC) cells. In vivo, KB-0742 (60 mg/kg) reduces tumor volume in the MYC-amplified CTG-0437 patient-derived xenograft (PDX) mouse model of TNBC.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Freeman, D.B., Hopkins, T.D., Mikochik, P.J., et al. Discovery of KB-0742, a potent, selective, orally bioavailable small molecule inhibitor of CDK9 for MYC-dependent cancers. J. Med. Chem. 66(23), 15629-15647 (2023).