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SSR128129E

Synonyms: SSR

Catalog No.S7167 Purity: 99.93%

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

SSR128129E Chemical Structure

CAS: 848318-25-2

Selleck's SSR128129E has been cited by 9 Publications

2 Customer Reviews

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

Related Targets	FGFR1 FGFR2 FGFR3 FGFR4	Click to Expand
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Signaling Pathway

FGFR Signaling Pathway

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
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
Kinase Assay	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05974293	Not yet recruiting	NMO Spectrum Disorder\|Spasticity Muscle	Michael Levy M.D.Ph.D.\|Jazz Pharmaceuticals\|Massachusetts General Hospital	April 2024	Phase 2
NCT05660239	Not yet recruiting	Epilepsy	Makerere University\|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)\|Duke University	March 2024	Not Applicable
NCT06191289	Not yet recruiting	Suicide	University of Illinois at Chicago	February 20 2024	Early Phase 1
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)	February 1 2024	Not Applicable

References
[1] Bono F, et al. Cancer Cell. 2013, 23(4), 477-488. [2] Dol-Gleizes F, et al. PLoS One. 2013, 8(11), e80027.

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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