GS-9901

A PI3Kdelta inhibitor (IC50 = 1 nM), selective for PI3Kdelta over PI3Kalpha, PI3Kbeta, and PI3Kgamma (IC50s = 750, 100, and 190 nM, respectively) and a panel of 456 additional kinases, including 11 lipid and 56 mutant kinases, at 10 µM, activates basophils in isolated human whole blood (EC50 = 1 nM), decreases ankle swelling and disease severity in a rat model of collagen-induced arthritis at 1 and 3 mg/kg. Formulation: A solid. InChI: InChI=1S/C22H17ClFN9O/c23-13-5-6-14(24)17-15(13)21(34)33(11-2-1-7-28-9-11)20(30-17)16(10-3-4-10)29-19-12(8-25)18(26)31-22(27)32-19/h1-2,5-7,9-10,16H,3-4H2,(H5,26,27,29,31,32)/t16-/m0/s1. InChIKey: XDSXYMOZKDUASY-INIZCTEOSA-N. SMILES: N#CC(C(N[C@@H](C1CC1)C(N(C2=CN=CC=C2)C(C3=C(Cl)C=C4)=O)=NC3=C4F)=NC(N)=N5)=C5N