PFK158

PFK158 is an inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3, IC50 = 137 nM for human recombinant PFKFB3). It inhibits PFKFB3 and glycolysis in Jurkat cells (IC50s = 1.6 and 0.847 µM, respectively). PFK158 inhibits the growth of leukemia cells in vitro (IC50 = 0.33 µM for Jurkat cells) and reduces tumor volume in CT-26 murine colon carcinoma syngeneic model and a BxPC-3 pancreatic cancer mouse xenograft model. PFK158 also enhances activity of the anti-CTLA-4 antibody in the B16/F10 mouse model of melanoma.Formal Name: 1-(4-pyridinyl)-3-[7-(trifluoromethyl)-2E-quinolinyl]-2-propen-1-one. CAS Number: 1462249-75-7. Molecular Formula: C18H11F3N2O. Formula Weight: 328.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 33 mg/ml, DMF:PBS(pH7.2) (1:2): 0.3 mg/ml, DMSO: 1 mg/ml. lambdamax: 280, 323 nm. SMILES: O=C(/C=C/C1=NC(C=C(C(F)(F)F)C=C2)=C2C=C1)C3=CC=NC=C3. InChi Code: InChI=1S/C18H11F3N2O/c19-18(20,21)14-3-1-12-2-4-15(23-16(12)11-14)5-6-17(24)13-7-9-22-10-8-13/h1-11H/b6-5+. InChi Key: IAJOMYABKVAZCN-AATRIKPKSA-N.