SSR128129E

Catalog No.S7167 Synonyms: SSR

SSR128129E Chemical Structure

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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2 Customer Reviews

  • 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

Biological Activity

Description SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 μM, while not affecting other related RTKs.
Targets
FGFR1 [1]
1.9 μM
In vitro

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. [1]

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. [1] SSR128129E also inhibits arteriosclerosis in a mouse vein graft model and atherosclerosis in apolipoprotein E-deficient mice. [2]

Protocol

Kinase Assay:

[1]

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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.
Cell Research:

[1]

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  • Cell lines: Endothelial cells (ECs) and Panc02 tumor cells
  • Concentrations: ~100 nM
  • Incubation Time: 72 hours
  • Method:

    Cell proliferation of porcine aortic endothelial (PAE) and tumor cell lines is analyzed on exponentially growing cells that are starved for 16 hours in 0.2 % FBS containing medium and seeded at 4,000 cells/well in 96-well microplates. After exposure to mitogens and/or SSR for 72 hours, cell proliferation is assessed with the use of the CellTiter 96 AQueous One Solution Cell Proliferation Assay according to manufacturer’s instructions. 10 % FBS containing medium is used a positive control.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Mouse model of Arthritic and mouse tumor model bearing pancreatic tumor cell line Panc02, murine mammary carcinoma cell line 4T1, murine colon cancer cell line CT26, or human breast MCF7/ADR cell line.
  • Formulation: 0.6 % methylcellulose
  • Dosages: ~30 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 69 mg/mL (199.24 mM)
Water 1 mg/mL (2.88 mM)
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 346.31
Formula

C18H15N2O4.Na

CAS No. 848318-25-2
Storage powder
Synonyms SSR

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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
NCT02497612 Recruiting Plasmodium Falciparum Infection Sanofi July 2015 Phase 2
NCT02387905 Recruiting Spinal Cord Diseases M.D. Anderson Cancer Center|High Impact Clinical Research Support Program March 2015 Phase 2
NCT02279953 Completed Major Depressive Disorder H. Lundbeck A/S October 2014 Phase 3
NCT01439919 Terminated Pain|Breakthrough Cancer Pain Sanofi January 2012 Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID