GSK2837808A

GSK2837808A is a potent inhibitor of lactate dehydrogenase (LDH) A and B (IC50s = 2.6 and 0.43 nM, for human recombinant LDHA and LDHB, respectively). It inhibits lactate production in Snu398 hepatocellular carcinoma cells in which LDHB expression is undetectable (EC50 = 400 nM). GSK2837808A (10 µM) reduces glucose consumption in Snu398 but not HepG2 hepatocellular carcinoma cells. A panel of 30 cancer cell lines, with varying levels of LDHA and LDHB expression, shows differential sensitivities to GSK2837808A with EC50s ranging from 400 nM to 30 µM. The potency of GSK2837808A does not correlate with LDHA, LDHB, or total LDH expression levels.Formal Name: 3-[[3-[(cyclopropylamino)sulfonyl]-7-(2,4-dimethoxy-5-pyrimidinyl)-4-quinolinyl]amino]-5-(3,5-difluorophenoxy)-benzoic acid. CAS Number: 1445879-21-9. Molecular Formula: C31H25F2N5O7S. Formula Weight: 649.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml, Ethanol: slightly soluble. lambdamax: 223, 266 nm. SMILES: FC1=CC(F)=CC(OC2=CC(C(O)=O)=CC(NC3=C(S(NC4CC4)(=O)=O)C=NC5=C3C=CC(C6=C(OC)N=C(OC)N=C6)=C5)=C2)=C1. InChi Code: InChI=1S/C31H25F2N5O7S/c1-43-29-25(14-35-31(37-29)44-2)16-3-6-24-26(9-16)34-15-27(46(41,42)38-20-4-5-20)28(24)36-21-7-17(30(39)40)8-22(13-21)45-23-11-18(32)10-19(33)12-23/h3,6-15,20,38H,4-5H2,1-2H3,(H,34,36)(H,39,40). InChi Key: RZBCPMYJIARMGV-UHFFFAOYSA-N.