SSR128129E

Catalog No.S7167 Synonyms: SSR

For research use only.

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 No. 848318-25-2

Selleck's SSR128129E has been cited by 9 Publications

2 Customer Reviews

Purity & Quality Control

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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]

Assay
Methods Test Index PMID
Western blot pFGFR1 / FGFR1 / pERK / ERK / NANOG 28092370
Growth inhibition assay Cell viability 28092370
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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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.

Animal Research:

[1]

  • 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

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 346.31
Formula

C18H15N2O4.Na

CAS No. 848318-25-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(N2C=CC=CC2=C1OC)C(=O)C3=CC(=C(C=C3)N)C(=O)[O-].[Na+]

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

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Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05156112 Not yet recruiting Device: Positive Airway Pressure Device Post Traumatic Stress Disorder|Obstructive Sleep Apnea|Substance Use Disorder|Residential Treatment Program VA Office of Research and Development April 1 2022 Not Applicable
NCT04950608 Not yet recruiting Drug: Psilocybin|Behavioral: Psychotherapy Hospice|Psilocybin|Demoralization|Terminal Illness|Cancer-related Problem/Condition|Psychotherapy|Terminal Cancer|Cancer Terminal Yvan Beaussant|Oppenheimer Family Psychosocial Oncology and Palliative Care Research Grants|Usona Institute|Carey and Claudia Turnbull Family Foundation|Heffter Research Institute|George Sarlo Foundation|RiverStyx Foundation|Council on Spiritual Practices Fund at the San Francisco Foundation|Nikean Foundation|Jack Smith|Dana-Farber Cancer Institute February 2022 Phase 2
NCT05156827 Not yet recruiting Drug: TB006|Drug: Placebo Acute Ischemic Stroke TrueBinding Inc. February 15 2022 Phase 2
NCT05127330 Not yet recruiting Behavioral: LifePlans|Behavioral: Treatment as Usual Suicidal Ideation|Suicidal Behaviors|Suicide Butler Hospital January 1 2022 Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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