Home Angiogenesis FGFR inhibitor SSR128129E For research use only.

SSR128129E

Synonyms: SSR

SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 μM, while not affecting other related RTKs.

SSR128129E Chemical Structure

SSR128129E Chemical Structure

CAS No. 848318-25-2

Purity & Quality Control

Batch: S716701 DMSO]69 mg/mL]false]Water]1 mg/mL]false]Ethanol]Insoluble]false Purity: 99.93%
99.93

SSR128129E Related Products

Signaling Pathway

FGFR Signaling Pathways

FGFR Signaling Pathway

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
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]
Kinase Assay 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 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot pFGFR1 / FGFR1 / pERK / ERK / NANOG 28092370
Growth inhibition assay Cell viability 28092370
In Vivo
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]
Animal Research 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.
Dosages ~30 mg/kg
Administration Oral administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06194331 Not yet recruiting
Suicidal Ideation|Suicidal and Self-injurious Behavior|Depression
University of Pittsburgh|Pediatric Research in Office Settings|National Institute of Mental Health (NIMH)
 December 1 2024 Not Applicable
NCT06175767 Not yet recruiting
Parkinson''s Disease
Mthera Pharma Co. Ltd.
 July 2024 Phase 2
NCT03575000 Not yet recruiting
Schizophrenia|PreDiabetes
VA Pittsburgh Healthcare System
 July 1 2024 Phase 4

Chemical Information & Solubility

Molecular Weight 346.31 Formula

C18H15N2O4.Na
CAS No. 848318-25-2 SDF Download SSR128129E SDF
Smiles CC1=C(N2C=CC=CC2=C1OC)C(=O)C3=CC(=C(C=C3)N)C(=O)[O-].[Na+]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 69 mg/mL ( (199.24 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 1 mg/mL

Ethanol : Insoluble


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In vivo
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Tech Support

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.

Handling Instructions

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