KI-ARv-03

KI-ARv-03 is a potent and selective ATP-competitive CDK9 inhibitor with an IC₅₀ of 0.15 μM (at 45 μM ATP), exhibiting over 130-fold selectivity against other CDKs (including CDK1-7) . KI-ARv-03 reduces androgen receptor (AR) -driven transcription and proliferation in prostate cancer cells. KI-ARv-03 can be used for leukemia, pancreatic cancer, alveolar rhabdomyosarcoma (ARMS) and castration-resistant prostate cancer (CRPC) research. KI-ARv-03 is a ligand for target protein for PROTAC. KI-ARv-03 can be used to synthesize PROTAC KI-CDK9d-32 (HY-173523) [1][2].

Product Specifications

CAS Number

[2416873-72-6]

UNSPSC

12352005

Target

CDK; c-Myc; Ligands for Target Protein for PROTAC

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; PROTAC

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

CCCC1=NC2=CC=NN2C(N[C@H]3C[C@@H](CC3)N)=C1

Molecular Formula

C14H21N5

Molecular Weight

259.35

References & Citations

[1]Richters A, et al. Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors. Cell Chem Biol. 2021 Feb 18;28 (2) :134-147.e14|[2]Toure MA, et al. Targeted degradation of CDK9 potently disrupts the MYC-regulated network. Cell Chem Biol. 2025 Apr 17;32 (4) :542-555.e10.