Alofanib

Alofanib is an allosteric inhibitor of FGFR2. It inhibits FGF2-induced phosphorylation of FGFR substrate 2 (FRS2alpha) in KATO III gastric carcinoma cells (IC50 = 50s = 370 and 210 nM, respectively). It inhibits proliferation of human umbilical vein endothelial cells (HUVECs) induced by basic FGF (bFGF, IC50 = 11 nM) and tube formation of SVEC4-10 endothelial cells when used at a concentration of 50 nM. It also inhibits migration of SVEC4-10 cells in a wound healing assay. Alofanib (50 mg/kg) decreases the number of microvessels in tumor tissue by 50% in a SKOV3 ovarian serous carcinoma mouse model. It reduces tumor growth in mouse xenograft models when administered at a dose of 30 mg/kg per day, and the degree of tumor volume reduction positively correlates with the expression level of FGFR2Formal Name: 3-[[[4-methyl-2-nitro-5-(3-pyridinyl)phenyl]amino]sulfonyl]-benzoic acid. CAS Number: 1612888-66-0. Synonyms: RPT835. Molecular Formula: C19H15N3O6S. Formula Weight: 413.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml, PBS (pH 7.2): slightly soluble. SMILES: O=C(C1=CC=CC(S(=O)(NC2=C([N+]([O-])=O)C=C(C)C(C3=CN=CC=C3)=C2)=O)=C1)O. InChi Code: InChI=1S/C19H15N3O6S/c1-12-8-18(22(25)26)17(10-16(12)14-5-3-7-20-11-14)21-29(27,28)15-6-2-4-13(9-15)19(23)24/h2-11,21H,1H3,(H,23,24). InChi Key: QUQGQIASFYWKAB-UHFFFAOYSA-N.