Acalisib

Acalisib is an inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) catalytic subunit p110delta (IC50 = 12.7 nM). It is selective for p110delta over the class I PI3K subunits p110alpha, p110beta, p110gamma, the class II PI3K CIIbeta, and the class III PI3K hVPS34 (IC50s = 5.4, 3.3, 1.4, 10, and 12.6 µM, respectively), as well as PIP5Kalpha, PIP5Kbeta, 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 (Cay-16665) in vitro and reduces tumor growth when administered in combination with melphalan in an LAGk-2 mouse xenograft model.Formal Name: 6-fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)ethyl]-4(3H)-quinazolinone. CAS Number: 870281-34-8. Synonyms: GS-9820. Molecular Formula: C21H16FN7O. Formula Weight: 401.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. lambdamax: 268 nm. SMILES: C[C@@H](C1=NC(C=CC(F)=C2)=C2C(N1C3=CC=CC=C3)=O)NC4=C5C(N=CN5)=NC=N4. InChi Code: InChI=1S/C21H16FN7O/c1-12(27-19-17-18(24-10-23-17)25-11-26-19)20-28-16-8-7-13(22)9-15(16)21(30)29(20)14-5-3-2-4-6-14/h2-12H,1H3,(H2,23,24,25,26,27)/t12-/m0/s1. InChi Key: DOCINCLJNAXZQF-LBPRGKRZSA-N.