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SSR128129E

Catalog No.
B1525
allosteric inhibitor of FGFR1, orally-active
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$127.00
In stock
5mg
$68.00
In stock
20mg
$189.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt346.31
Cas No.848318-25-2
FormulaC18H15N2O4·Na
Solubilityinsoluble in EtOH; insoluble in H2O; ≥17.3 mg/mL in DMSO
Chemical Namesodium;2-amino-5-(1-methoxy-2-methylindolizine-3-carbonyl)benzoate
SDFDownload SDF
Canonical SMILESCC1=C(N2C=CC=CC2=C1OC)C(=O)C3=CC(=C(C=C3)N)C(=O)[O-].[Na+]
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

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