Formulation: A solid
Formal Name: 5-[2-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-8-(4-morpholinyl)imidazo[1,2-a]pyrazin-6-yl]-2-pyrimidinamine
Purity: ≥98%
Formula Markup: C20H27N9O3S
Formula Weight: 473,6
Shelf life (days): 1460
CAS Number: 1252594-99-2
Notes: ETP-46321 is an inhibitor of PI3K p110α and p110δ (apparent Kis = 2.3 and 14.2 nM, respectively).{66300} It is selective for PI3K p110α and p110δ over p110β and p110γ (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.{66301}