6-Cyclohexylmethoxy-2-(4′-sulfamoylanilino)purine White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A 2,6-disubstituted purine compound that displays antiproliferative properties. Acts as a potent and ATP-competitive inhibitor of Cdk1/cyclin B and Cdk2/cyclin A3 (IC50 = 9.5 nM and 5.4 nM). Displays greater selectivity for Cdk1/2 over other kinases tested (IC50 = 600 nM, 800 nM, 900 nM and 1.6 µM for ROCKII, PDK1, DYRK1A and Cdk4/D1, respectively). Shown to inhibit human MCF-7 breast carcinoma cell growth with a GI50 of 8 µM. Purity: ≥95% by HPLC. Ref.: Hardcastle, I.R., et al. 2004. J. Med. Chem. 47, 3710. Sayle, K.L., et al. 2003. Bioorg. Med. Chem. Lett. 13, 3079. Davies, T.G., et al. 2002. Nat. Struct. Biol. 9, 745. |
