Name | AZ 6102 |
---|---|
Supplier | Tocris Bioscience |
Catalog | 3994 |
Prices | $199.00, $825.00 |
Sizes | 10 mg, 50 mg |
Function Type | Inhibitor |
Cas Number | 1645286-75-4 |
Chemical Name | rel-2-[4-[6-[(3R,5S)-3,5-Dimethyl-1-piperazinyl]-4-methyl-3-pyridinyl]phenyl]-3,7-dihydro-7-methyl-4H-pyrrolo[2,3-d]pyrimidin-4-one |
Formula | C25H28N6O |
Molecular Weight | 428.53 |
Purity | >98 % |
Description | Potent TNKS2 and TNKS1 inhibitor (IC 50 values are 1 and 3 nM, respectively). Exhibits >100-fold selectivity for TNKS1/2 over PARP-1, PARP-2 and PARP-6. Inhibits Wnt signaling in DLD-1 cells (IC 50 = 5 nM). Exhibits moderate oral bioavailability. |
Supplier Page | Shop |
Khazak V, Astsaturov I, Serebriiskii IG, Golemis EA. Expert Opin Ther Targets. 2007 Dec;11(12):1587-609.
Montagut C, Sharma SV, Shioda T, McDermott U, Ulman M, Ulkus LE, Dias-Santagata D, Stubbs H, Lee DY, Singh A, Drew L, Haber DA, Settleman J. Cancer Res. 2008 Jun 15;68(12):4853-61.
Hatzivassiliou G, Song K, Yen I, Brandhuber BJ, Anderson DJ, Alvarado R, Ludlam MJ, Stokoe D, Gloor SL, Vigers G, Morales T, Aliagas I, Liu B, Sideris S, Hoeflich KP, Jaiswal BS, Seshagiri S, Koeppen H, Belvin M, Friedman LS, Malek S. Nature. 2010 Mar 18;464(7287):431-5.