CAN508 is a potent, selective CDK9 inhibitor with IC50 of 0.35 uM (CDK9/cyclin T1), displays >35 fold selectivity over CDK1/2/4/7 (IC50=13.5-70 uM).
CAN508 reduces the frequency of S-phase cells of the cancer cell line HT-29 in antiproliferation assays.
CAN508 decreases phosphorylation of the retinoblastoma protein and the C-terminal domain of RNA polymerase II, inhibits mRNA synthesis, and induces the tumor suppressor protein p53.
Physicochemical Properties
M.Wt
218.22
Formula
C9H10N6O
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
4-[(3,5-diamino-1H-pyrazol-4-yl)azo]-phenol
References
1. Krystof V, et al. J Med Chem. 2006 Nov 2;49(22):6500-9.
2. Kryštof V, et al. Eur J Med Chem. 2011 Sep;46(9):4289-94.
3. Tong Z, et al. Oncotarget. 2017 Apr 25;8(17):28696-28710.
