KB-0742 (dihydrochloride)

KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity[1][2].

Product Specifications

CAS Number

[2416874-75-2]

UNSPSC

12352005

Target

CDK

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/kb-0742-dihydrochloride.html

Concentration

10mM

Purity

98.77

Solubility

DMSO : 62.5 mg/mL (ultrasonic) |H2O : 100 mg/mL (ultrasonic)

Smiles

N[C@@H]1C[C@@H](NC2=CC(C(CC)CC)=NC3=CC=NN23)CC1.[H]Cl.[H]Cl

Molecular Formula

C16H27Cl2N5

Molecular Weight

360.33

References & Citations

[1]André Richters, et al. Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors. Cell Chem Biol. 2020 Oct 20; S2451-9456 (20) 30380-9.|[2]Freeman DB, et al. Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9 for MYC-Dependent Cancers. J Med Chem. 2023 Dec 14;66 (23) :15629-15647.