SSR 128129E

SSR 128129E is a potent inhibitor of the FGF receptor (FGFR, IC50 = 1.9 nM). It reduces FGF2-induced endothelial cell proliferation and migration (IC50s = 31 and 15.2 nM, respectively), as well as lamellipodia formation in vitro. SSR 128129E also reduces proliferation of PAE cells expressing FGFR1, mPanc02 cells expressing FGFR2, hB9 myeloma cells expressing FGFR3, and HUVECs expressing FGFR4 when used at a concentration of 100 nM. In vivo, SSR 128129E (30 mg/kg per day) reduces limb swelling, redness, and deformity and improves performance in an exercise endurance test in a mouse model of arthritis. It reduces tumor growth and metastasis and enhances antitumor activity of the VEGF receptor (VEGFR) antibody alphaVEGFR2 in a Panc02 mouse orthotopic tumor model. SSR 128129E (50 mg/kg per day) reduces atherosclerotic lesion size in the aortic sinus of apoE-/- mice. It also reduces intimal hyperplasia following jugular vein-to-artery bypass grafting surgery in rats.Formal Name: 2-amino-5-[(1-methoxy-2-methyl-3-indolizinyl)carbonyl]-benzoic acid, monosodium salt. CAS Number: 848318-25-2. Molecular Formula: C18H15N2O4 . Na. Formula Weight: 346.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 1 mg/ml, PBS (pH 7.2): 1 mg/ml. lambdamax: 219, 238, 406 nm. SMILES: NC1=C(C([O-])=O)C=C(C(C2=C(C)C(OC)=C3N2C=CC=C3)=O)C=C1.[Na+]. InChi Code: InChI=1S/C18H16N2O4.Na/c1-10-15(20-8-4-3-5-14(20)17(10)24-2)16(21)11-6-7-13(19)12(9-11)18(22)23,/h3-9H,19H2,1-2H3,(H,22,23),/q,+1/p-1. InChi Key: JFBMSTWZURKQOC-UHFFFAOYSA-M.