An FGFR inhibitor (IC50 = 1.9 nM); reduces FGF2-induced endothelial cell proliferation and migration (IC50s = 31 and 15.2 nM

SSR 128129E – 1 mg

Brand:
Cayman
CAS:
848318-25-2
Storage:
-20
UN-No:
Non-Hazardous - /

SSR 128129E is a potent inhibitor of the FGF receptor (FGFR; IC50 = 1.9 nM).{42030} 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 αVEGFR2 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.{42031} It also reduces intimal hyperplasia following jugular vein-to-artery bypass grafting surgery in rats.{42032}  

 

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Description

An FGFR inhibitor (IC50 = 1.9 nM); reduces FGF2-induced endothelial cell proliferation and migration (IC50s = 31 and 15.2 nM, respectively); reduces proliferation of cells expressing FGFR1-4 at 100 nM; reduces disease severity and enhances physical performance in a mouse model of arthritis at 30 mg/kg per day; reduces tumor growth and metastasis in a Panc02 mouse orthotopic tumor model; reduces atherosclerotic lesion size in the aortic sinus of apoE-/- mice at 50 mg/kg per day; 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

Synonyms: 

Molecular weight: 346.3

CAS: 848318-25-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|FGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cardiovascular System|Cardiovascular Diseases|Atherosclerosis||Research Area|Cardiovascular System|Lipids & Lipoproteins|Lipoproteins||Research Area|Cardiovascular System|Vasculature|Angiogenesis||Research Area|Cardiovascular System|Vasculature|Endothelium||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis

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