产品描述:
Acalisib is an inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) catalytic subunit p110δ (IC50 = 12.7 nM).{42484} It is selective for p110δ over the class I PI3K subunits p110α, p110β, p110γ, the class II PI3K CIIβ, and the class III PI3K hVPS34 (IC50s = 5.4, 3.3, 1.4, 10, and 12.6 μM, respectively), as well as PIP5Kα, PIP5Kβ, DNA-PK, and mTOR (IC50s = >10 μM). Acalisib (1 μM) reduces lamellipodia spreading and induces lamellipodia retraction in rat osteoclasts. It reduces proliferation of multiple myeloma tumor cells alone and in combination with melphalan (Item No. 16665) in vitro and reduces tumor growth when administered in combination with melphalan in an LAGk-2 mouse xenograft model.{42483}