ETP-46321

ETP-46321 is an inhibitor of PI3K p110alpha and p110delta (apparent Kis = 2.3 and 14.2 nM, respectively). It is selective for PI3K p110alpha and p110delta over p110beta and p110gamma (apparent Kis = 170 and 179 nM, respectively), as well as a panel of 288 kinases at 1 µM. ETP-46321 inhibits Akt phosphorylation in U2OS cells (IC50 = 8.3 nM). In vivo, ETP-43621 (50 mg/kg) reduces tumor volume in a K-RasG12V-driven murine lung tumor model. It also reduces anti-collagen IgG1 and IgG2a production, swelling, and joint rigidity in a mouse model of collagen-induced arthritis.Formal Name: 5-[2-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-8-(4-morpholinyl)imidazo[1,2-a]pyrazin-6-yl]-2-pyrimidinamine. CAS Number: 1252594-99-2. Molecular Formula: C20H27N9O3S. Formula Weight: 473.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml. lambdamax: 270 nm. SMILES: O=S(N1CCN(CC1)CC2=CN3C=C(C4=CN=C(N)N=C4)N=C(N5CCOCC5)C3=N2)(C)=O. InChi Code: InChI=1S/C20H27N9O3S/c1-33(30,31)29-4-2-26(3-5-29)12-16-13-28-14-17(15-10-22-20(21)23-11-15)25-19(18(28)24-16)27-6-8-32-9-7-27/h10-11,13-14H,2-9,12H2,1H3,(H2,21,22,23). InChi Key: OHKDVDMWRKFZRB-UHFFFAOYSA-N.