848318-25-2

Basic information

• Product Name: FGFR inhibitor
• Synonyms: SSR128129E;Sodium 2-amino-5-[(1-methoxy-2-methylindolizin-3-yl)carbonyl]benzoate;Benzoic acid, 2-amino-5-[(1-methoxy-2-methyl-3-indolizinyl)carbonyl]-, sodium salt (1:1);Sodium 2-amino-5-[(1-methoxy-2-methylindolizin-3-yl)carbonyl]benzoate SSR128129E;Sodium 2-amino-5-(1-methoxy-2-methylindolizine-3-carbonyl)benzoate
• CAS NO: 848318-25-2
• Molecular Formula: C18H15N2NaO4
• Molecular Weight: 346.31247
• Product Categories: Inhibitors
• Mol File: 848318-25-2.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• Storage Temp.: Hygroscopic, -20°C Freezer, Under inert atmosphere
• Solubility: DMSO (Slightly), Methanol (Slightly)
• CAS DataBase Reference: FGFR inhibitor(CAS DataBase Reference)
• NIST Chemistry Reference: FGFR inhibitor(848318-25-2)
• EPA Substance Registry System: FGFR inhibitor(848318-25-2)

Safety Data

• Hazardous Substances Data: 848318-25-2(Hazardous Substances Data)

Usage

Description

FGFR inhibitor, specifically SSR128129E (SSR), is a potent pharmaceutical compound that targets and inhibits the fibroblast growth factor receptor (FGFR). This inhibition plays a crucial role in managing various pathological conditions by regulating cell growth and division.

Uses

Used in Pharmaceutical Industry:
FGFR inhibitor is used as a therapeutic agent for treating conditions characterized by abnormal cell growth and division. Its ability to inhibit FGFR makes it a promising candidate for addressing diseases such as cancer and arthritis.
FGFR inhibitor is used as an anti-arthritis agent for managing arthritis symptoms. Oral delivery of SSR128129E has been shown to effectively inhibit arthritis, providing relief and improving the quality of life for patients suffering from this condition.
FGFR inhibitor is also used as an anti-tumor agent for combating tumors that are relatively refractory to anti-vascular endothelial growth factor receptor-2 antibodies. By targeting the FGFR pathway, SSR128129E can potentially overcome resistance to other treatments and offer a novel approach to cancer therapy.

Biological Activity

ssr128129e is an allosteric inhibitor of fgfr1 with ic50 value of 1.9 μm [1].the fibroblast growth factor receptors (fgfrs) are receptor tyrosine kinases for fibroblast growth factors (fgfs) and play an important role in cancer and inflammation. fgf2 plays an important role in angiogenesis [1] [2].ssr128129e is an orally-active and allosteric fgfr1 inhibitor. in human umbilical venous endothelial cells (huvecs), ssr128129e inhibited fgf2-induced endothelial cells (ecs) proliferation and migration with ic50 values of 31 and 15.2 nm respectively and also inhibited lamellipodia formation. ssr128129e inhibited responses mediated by fgfr1-4. in fgfr2-expressing hek293 cells, ssr128129e inhibited phosphorylation of frs2 and erk1/2 induced by fgf2 [1].in arthritis mice, ssr128129e inhibited bone and joint damage and reduced angiogenesis in the inflamed joints. in orthotopic panc02 tumor model, ssr128129e (30 mg/kg) inhibited tumor growth by 44%. in murine 4t1 breast tumors, ssr128129e (30 mg/kg) reduced tumor weight and size by 40% and 53%, respectively [1]. in atherosclerosis-prone apolipoprotein e (apoe)-deficient mice, ssr128129e (50 mg/kg) reduced neointimal proliferation and reduced fgfr2 mrna levels and lesion size in the aortic sinus [2].

references

[1]. bono f, de smet f, herbert c, et al. inhibition of tumor angiogenesis and growth by a small-molecule multi-fgf receptor blocker with allosteric properties. cancer cell, 2013, 23(4): 477-488.[2]. dol-gleizes f, delesque-touchard n, marès am, et al. a new synthetic fgf receptor antagonist inhibits arteriosclerosis in a mouse vein graft model and atherosclerosis in apolipoprotein e-deficient mice. plos one, 2013, 8(11): e80027.