RGB-286147

• CAT Number: R066926
• CAS Number: 784211-09-2
• Molecular Formula: C23H22Cl2N4O3
• Molecular Weight: 473.35
• Purity: ≥95%
• Synonyms: 1-(2,6-dichlorophenyl)-6-[[4-(2-hydroxyethoxy)phenyl]methyl]-3-propan-2-yl-5H-pyrazolo[3,4-d]pyrimidin-4-one
• InChI: InChI=1S/C23H22Cl2N4O3/c1-13(2)20-19-22(29(28-20)21-16(24)4-3-5-17(21)25)26-18(27-23(19)31)12-14-6-8-15(9-7-14)32-11-10-30/h3-9,13,30H,10-12H2,1-2H3,(H,26,27,31)
• InChIKey: RSQPNXBTPUXMQN-UHFFFAOYSA-N
• SMILES: CC(C)C1=NN(C2=C1C(=O)NC(=N2)CC3=CC=C(C=C3)OCCO)C4=C(C=CC=C4Cl)Cl

RGB-286147 is a selective and ATP-competitive CDK and CDK-related kinases (CRK) inhibitor with IC50 values ranging from 9-839 nM. RGB-286147 shows less active against other non-CDK/CRK kinases. RGB-286147 induces cell apoptosis, and exhibits anti-tumor activity[1].
RGB-286147 (50-100 nM; 24-48 hr) induces cell cycle arrest in the G1 phase, causes a marked inhibition of DNA replication, and induces apoptosis in HCT116 cells[1].
RGB-286147 (100 nM; 48 hr) results in proteolytic cleavage of PARP in HCT116 cells[1].
RGB-286147 (24-72 hr) shows potent and irreversible cell killing activity in HCT116 cells. The IC50 value for inhibition of colony formation by RGB-286147 is 57 nM[1].
RGB-286147 (48 hr) exhibits broad anti-tumor activity with an average GI50 value of <10 nM for 60 tumorigenic cell lines. And also inhibits growth of non-cycling HCT116 cells with an IC50 value of 40 nM[1].

Reference

[1]. Maureen Caligiuri, et al. A proteome-wide CDK/CRK-specific kinase inhibitor promotes tumor cell death in the absence of cell cycle progression. Chem Biol. 2005 Oct;12(10):1103-15.
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