WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406387
CAS#: 848318-25-2
Description: SSR128129E (SSR) is an potent FGFR inhibitor, which inhibits fibroblast growth factor receptor (FGFR) signaling by binding to the extracellular FGFR domain without affecting orthosteric FGF binding. SSR128129E exhibits allosteric properties, including probe dependence, signaling bias, and ceiling effects. Inhibition by SSR128129E is highly conserved throughout the animal kingdom. Oral delivery of SSR128129E inhibits arthritis and tumors that are relatively refractory to anti-vascular endothelial growth factor receptor-2 antibodies. Thus, orally-active extracellularly acting small-molecule modulators of RTKs with allosteric properties can be developed and may offer opportunities to improve anticancer treatment.
MedKoo Cat#: 406387
Name: SSR128129E
CAS#: 848318-25-2
Chemical Formula: C18H16N2O4
Exact Mass: 324.11101
Molecular Weight: 324.33
Elemental Analysis: C, 66.66; H, 4.97; N, 8.64; O, 19.73
Synonym: SSR128129E; SSR 128129E; SSR-128129E.
IUPAC/Chemical Name: sodium 2-amino-5-(1-methoxy-2-methylindolizine-3-carbonyl)benzoate
InChi Key: JFBMSTWZURKQOC-UHFFFAOYSA-M
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
SMILES Code: O=C([O-])C1=CC(C(C2=C(C)C(OC)=C3C=CC=CN23)=O)=CC=C1N.[Na+]
1: Dol-Gleizes F, Delesque-Touchard N, Marès AM, Nestor AL, Schaeffer P, Bono F. A New Synthetic FGF Receptor Antagonist Inhibits Arteriosclerosis in a Mouse Vein Graft Model and Atherosclerosis in Apolipoprotein E-Deficient Mice. PLoS One. 2013 Nov 4;8(11):e80027. doi: 10.1371/journal.pone.0080027. PubMed PMID: 24224032; PubMed Central PMCID: PMC3817113.
2: Herbert C, Alcouffe C, Bono F. [SSR128129E, an extracellularly acting, small-molecule, allosteric inhibitor of FGF receptor signaling]. Med Sci (Paris). 2013 Oct;29(10):834-6. doi: 10.1051/medsci/20132910007. Epub 2013 Oct 18. French. PubMed PMID: 24148118.
3: Herbert C, Schieborr U, Saxena K, Juraszek J, De Smet F, Alcouffe C, Bianciotto M, Saladino G, Sibrac D, Kudlinzki D, Sreeramulu S, Brown A, Rigon P, Herault JP, Lassalle G, Blundell TL, Rousseau F, Gils A, Schymkowitz J, Tompa P, Herbert JM, Carmeliet P, Gervasio FL, Schwalbe H, Bono F. Molecular mechanism of SSR128129E, an extracellularly acting, small-molecule, allosteric inhibitor of FGF receptor signaling. Cancer Cell. 2013 Apr 15;23(4):489-501. doi: 10.1016/j.ccr.2013.02.018. PubMed PMID: 23597563.
4: Bono F, De Smet F, Herbert C, De Bock K, Georgiadou M, Fons P, Tjwa M, Alcouffe C, Ny A, Bianciotto M, Jonckx B, Murakami M, Lanahan AA, Michielsen C, Sibrac D, Dol-Gleizes F, Mazzone M, Zacchigna S, Herault JP, Fischer C, Rigon P, Ruiz de Almodovar C, Claes F, Blanc I, Poesen K, Zhang J, Segura I, Gueguen G, Bordes MF, Lambrechts D, Broussy R, van de Wouwer M, Michaux C, Shimada T, Jean I, Blacher S, Noel A, Motte P, Rom E, Rakic JM, Katsuma S, Schaeffer P, Yayon A, Van Schepdael A, Schwalbe H, Gervasio FL, Carmeliet G, Rozensky J, Dewerchin M, Simons M, Christopoulos A, Herbert JM, Carmeliet P. Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties. Cancer Cell. 2013 Apr 15;23(4):477-88. doi: 10.1016/j.ccr.2013.02.019. PubMed PMID: 23597562.
5: Mohan SK, Rani SG, Chiu IM, Yu C. WITHDRAWN: Interaction of FGF1 with a novel anti-angiogenic drug SSR128129E. Arch Biochem Biophys. 2012 Jun 5. [Epub ahead of print] PubMed PMID: 22683470.
