Catalog No.S7167 Synonyms: SSR
Molecular Weight(MW): 346.31
SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 μM, while not affecting other related RTKs.
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Western blot analysis of the expression and activation status (a) of pFGFR, pERK and Bim after treatment of API5-overexpressing cells (a) with either DMSO or SSR128129E.
Exp Mol Med, 2017, 49(9):e374. SSR128129E purchased from Selleck.
(a, d) Cells were treated with indicated concentrations of SSR128129E for 48 h. Cell viability was measured by an MTT assay, and then the concentrations resulting in 50% inhibition of cell viability (IC50 values) were determined. (b, e) Cells were treated with 10 μM of SSR128129E for 12 h. Expression levels of NANOG, pFGFR, FGFR, pERK and ERK in these cells were analyzed by western blot analysis. Numbers below blots indicate the expression as measured by fold change. (c, f) Cells were treated with 10 μM of SSR128129E for 12 h. Flow cytometry analysis of CD44 in these cells. Error bars represent mean±s.d. Data presented are representative of three independent experiments
Oncogenesis, 2017, 6(1):e285. SSR128129E purchased from Selleck.
Purity & Quality Control
Choose Selective FGFR Inhibitors
|Description||SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 μM, while not affecting other related RTKs.|
SSR128129E exhibits more effective activity in cell assay due to its allosteric mechanism. SSR128129E dose-dependently inhibits FGF2-induced EC proliferation and migration with IC50 of 31 nM and 15.2 nM, respectively. As a multi-FGFR inhibitor, SSR128129E inhibits responses mediated by FGFR1-4 and thus results in the blockage of proliferation and/or migration in various cell lines including mPanc02, HEK-hFGFR2WT, PAE-hFGFR1, hB9-myeloma and HUVEC. 
|In vivo||In Arthritis mice, SSR128129E (30 mg/kg, p.o.) inhibits angiogenesis, inflammation, and bone resorption, and reduces the severity of clinical symptoms. In mice bearing various tumor models, SSR128129E (30 mg/kg, p.o.) inhibits both the growth of primary tumors and metastasis. In addition, SSR128129E inhibits growth of anti-VEGFR2-refractory and -sensitive tumor models, and enhances the antitumor activity of anti-VEGFR2.  SSR128129E also inhibits arteriosclerosis in a mouse vein graft model and atherosclerosis in apolipoprotein E-deficient mice. |
Scintillation Proximity Assay, 125I-FGF-2 Binding:SPA protein A beads are supplied as a suspension in PBS at 20 mg/mL, then diluted with binding buffer (KCl, 400 mg/L; MgSO4 200 mg/L; NaCl 6.4 g/L; NaHCO3 3.7 g/L; NaH2PO4 0.141 mg/mL; bis Tris Propane 11.292 g/L; Glucose 4.5 g/L; Gelatin 0.1 %; pH 7.0) at 10 mg/mL. 125I-FGF-2 radioligand and FGFR-1IIIcß - Fc Chimera are diluted into binding buffer. Binding was performed on 96-well plates coated with 0.1 % gelatin. Total assay volume is 0.1 mL. Binding of 125I-FGF-2 is determined by incubation of SPA beads coated with protein A (0.5 mg/assay) with FGFR-1IIIcß - Fc chimera soluble receptor (5 ng/assay), FGF-2 (20 ng/assay) is used for non-specific binding determinations.
|In vitro||DMSO||69 mg/mL (199.24 mM)|
|Water||1 mg/mL (2.88 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02387905||Recruiting||Spinal Cord Diseases||M.D. Anderson Cancer Center|High Impact Clinical Research Support Program||March 9 2015||Phase 2|
|NCT03132103||Recruiting||Vitamin D Status||Bangor University|University of East Anglia|University of Manchester||January 6 2016||Not Applicable|
|NCT02497612||Recruiting||Plasmodium Falciparum Infection||Sanofi||July 25 2015||Phase 2|
|NCT02713269||Recruiting||Secondary Malignant Neoplasm of Vertebral Column|Spine Metastases||M.D. Anderson Cancer Center|Medtronic||August 2016||Phase 2|
|NCT02608866||Recruiting||Secondary Malignant Neoplasm of Spine||National Taiwan University Hospital||November 2015||Phase 2|
|NCT02279953||Completed||Major Depressive Disorder||H. Lundbeck A/S||October 2014||Phase 3|
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