GS-9973

Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that upon phosphorylation binds to immunoreceptor tyrosine-based activation motifs of FcRgamma chains and mediates downstream signaling related to platelet function and inflammation. GS-9973 is a potent Syk inhibitor (IC50 = 7.7 nM) that demonstrates 10-35-fold selectivity for Syk over a panel of 359 nonmutant kinases. In conjunction with the PI3Kdelta inhibitor CAL-101 (Cay-15279), it has been used to reduce chronic lymphocytic leukemia cell survival and to disrupt chemokine signaling at nanomolar concentrations.Formal Name: 6-(1H-indazol-6-yl)-N-[4-(4-morpholinyl)phenyl]-imidazo[1,2-a]pyrazin-8-amine. CAS Number: 1229208-44-9. Molecular Formula: C23H21N7O. Formula Weight: 411.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 15 mg/ml, DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml. lambdamax: 244, 328 nm. SMILES: C12=NC=CN1C=C(C3=CC=C(C=NN4)C4=C3)N=C2NC5=CC=C(N6CCOCC6)C=C5. InChi Code: InChI=1S/C23H21N7O/c1-2-17-14-25-28-20(17)13-16(1)21-15-30-8-7-24-23(30)22(27-21)26-18-3-5-19(6-4-18)29-9-11-31-12-10-29/h1-8,13-15H,9-12H2,(H,25,28)(H,26,27). InChi Key: XSMSNFMDVXXHGJ-UHFFFAOYSA-N.