RK-287107

RK-287107 is an inhibitor of the tankyrases TNKS1 and TNKS2 (IC50s = 0.014 and 0.010 µM, respectively). It is selective for TNKS1 and TNKS2 over poly(ADP-ribose) polymerase 1 (PARP1), PARP2, and PARP10 (IC50s = >20, 2.7, and 19.8 µM, respectively). RK-287107 inhibits Wnt-dependent signaling with an IC50 value of 0.077 µM in a reporter assay. It increases accumulation of Axin2, indicating inhibition of TNKS-mediated auto-PARsylation, in COLO 320DM colorectal cancer cells when used at a concentration of 0.1 µM. RK-287107 also inhibits cell growth in the same model (GI50 = 0.45 µM). It reduces tumor growth in a COLO 320DM mouse xenograft model when administered at a dose of 150 mg/kg twice per day.Formal Name: 2-[4,6-difluoro-1-(2-hydroxyethyl)spiro[3H-indole-3,4'-piperidine]-1'(2H)-yl]-5,6,7,8-tetrahydro-4(3H)-quinazolinone. CAS Number: 2171386-10-8. Molecular Formula: C22H26F2N4O2. Formula Weight: 416.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. lambdamax: 236, 298 nm. SMILES: O=C1N=C(NC2=C1CCCC2)N3CCC4(C(C(F)=CC(F)=C5)=C5N(CCO)C4)CC3. InChi Code: InChI=1S/C22H26F2N4O2/c23-14-11-16(24)19-18(12-14)28(9-10-29)13-22(19)5-7-27(8-6-22)21-25-17-4-2-1-3-15(17)20(30)26-21/h11-12,29H,1-10,13H2,(H,25,26,30). InChi Key: FZQYCOUBRJEYBC-UHFFFAOYSA-N.