GSK2126458

GSK2126458 is a potent inhibitor of phosphoinositide 3-kinase isoforms (Kis = 19, 130, 24, and 60 pM for p110alpha, beta, delta, and gamma, respectively). It also inhibits mTOR in both mTORC1 and mTORC2 (Kis = 180 and 300 nM, respectively), as well as several common mutant forms of p110alpha. GSK2126458 is orally bioavailable, displays favorable pharmacokinetics, and shows efficacy in tumor growth models. GSK2126458 positively combines with inhibitors of discoidin domain receptor 1 (DDR1) inhibitor DDR1-IN-1 (Cay-18092) to suppress the growth of SNU-1040 colorectal cancer cells.Formal Name: 2,4-difluoro-N-[2-methoxy-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl]-benzenesulfonamide. CAS Number: 1086062-66-9. Synonyms: GSK458, Omipalisib. Molecular Formula: C25H17F2N5O3S. Formula Weight: 505.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 5 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 225, 300 nm. SMILES: COC1=C(NS(C2=CC=C(F)C=C2F)(=O)=O)C=C(C3=CC(C(C4=CC=NN=C4)=CC=N5)=C5C=C3)C=N1. InChi Code: InChI=1S/C25H17F2N5O3S/c1-35-25-23(32-36(33,34)24-5-3-18(26)12-21(24)27)11-17(13-29-25)15-2-4-22-20(10-15)19(7-8-28-22)16-6-9-30-31-14-16/h2-14,32H,1H3. InChi Key: CGBJSGAELGCMKE-UHFFFAOYSA-N.