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SSR128129E

Cat. No. M3031
SSR128129E Structure
Synonym:

SSR

Size Price Availability Quantity
5mg USD 70  USD70 In stock
10mg USD 110  USD110 In stock
25mg USD 220  USD220 In stock
50mg USD 350  USD350 In stock
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Quality Control & Documentation
Biological Activity

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

Customer Product Validations & Biological Datas
Source PLoS One (2013). Figure 3. SSR128129E
Method qPCR
Cell Lines C57BL/6
Concentrations 50 mg/kg/d
Incubation Time -
Results Treatment of apoE-deficient mice with SSR128129E did not affect the mRNA levels of all the receptors but FGFR2, the levels of which were slightly, but significantly, reduced
Protocol (for reference only)
Cell Experiment
Cell lines Endothelial cells (ECs) and Panc02 tumor cells
Preparation 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, according to manufacturer’s instructions, assessing the cell proliferation with the use of the CellTiter 96 AQueous One Solution Cell Proliferation Assay . 10 % FBS containing medium is used a positive control
Concentrations ~100 nM
Incubation time 72 hours
Animal Experiment
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
Chemical Information
Molecular Weight 346.31
Formula C18H15N2O4.Na
CAS Number 848318-25-2
Solubility (25°C) DMSO 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Corentin Herbert, et al. Molecular Mechanism of SSR128129E, an Extracellularly Acting, Small-Molecule, Allosteric Inhibitor of FGF Receptor Signaling

[2] Isabelle Ader, et al. Preclinical evidence that SSR128129E--a novel small-molecule multi-fibroblast growth factor receptor blocker--radiosensitises human glioblastoma

[3] Corentin Herbert, et al. SSR128129E, an extracellularly acting, small-molecule, allosteric inhibitor of FGF receptor signaling

[4] Corentin Herbert, et al. Molecular mechanism of SSR128129E, an extracellularly acting, small-molecule, allosteric inhibitor of FGF receptor signaling

[5] Sepuru K Mohan, et al. WITHDRAWN: Interaction of FGF1 with a novel anti-angiogenic drug SSR128129E

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Keywords: SSR128129E, SSR supplier, FGFR, inhibitors, activators


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