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533434 FGFR Inhibitor, SSR128129E - CAS 848318-25-2 - Calbiochem

FGFR Inhibitor, SSR128129E, CAS 848318-25-2, is a highly potent, allosteric blocker of multi-fibroblast growth factor receptors. Inhibits selective responses mediated by FGFR1-4.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: FGFR Inhibitor, SSR

Primary Target: FGFR
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
848318-25-2C₁₈H₁₅N₂O₄Na

Products

Catalog NumberPackaging Qty/Pack
5.33434.0001 Glass bottle 10 mg
Description
OverviewAn orally bioavailable, highly potent allosteric blocker of multi-fibroblast growth factor receptors (FGFR) that specifically binds to the extracellular domain of the receptor and blocks selective responses mediated by FGFR1-4. Does not compete with FGF for binding to FGFR, but inhibits FGF-induced signaling linked to FGFR internalization. Also, does not show any binding to FGF1 or FGF2. Does not affect the activity of other related receptor tyrosine kinases. Shown to block the FGF2-induced ERK1/2 phosphorylation and prevent translocation of FGFR4 from cell surface to the cytosol, but does not block the phosphorylation of VEGFR2 or MET kinase. Inhibits FGF-1-innduced proliferation of HUVEC (IC50= 100 nM) and hB9-myeloma cells (IC50 = 25 nM) and diminishes FGF-2 induced ERK activation in HEKhFGFR2 WT (IC50 = 28 nM). Also reported to reduce the survival of endothelial cells in a dose-dependent manner (IC50 = 17.7 nM). Suppresses the growth of orthotopic Panc02 and 4T1 xenografts in mice (30 mg/kg/day, p.o) and delays the growth of Lewis lung carcinoma. Also shown to be effective against the multi-drug resistant MCF7/ADR breast cancer xenografts. Synergistically enhances the inhibitory effects of anti-VEGFR2.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Catalogue Number533434
Brand Family Calbiochem®
SynonymsFGFR Inhibitor, SSR
References
ReferencesDol-Gleizes, F., et al. 2013. Plos One. 8, e80027.
Herbert, C., et al. 2013. Cancer Cell. 23, 489.
Bono. F., et al. 2013. Cancer Cell. 23, 477.
Product Information
CAS number848318-25-2
FormYellow solid
Hill FormulaC₁₈H₁₅N₂O₄Na
Chemical formulaC₁₈H₁₅N₂O₄Na
Hygroscopic Hygroscopic
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary TargetFGFR
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Identification Number
Catalog Number GTIN
5.33434.00014055977286908

Documentation

FGFR Inhibitor, SSR128129E - CAS 848318-25-2 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

FGFR Inhibitor, SSR128129E - CAS 848318-25-2 - Calbiochem Certificates of Analysis

TitleLot Number
533434

References

Reference overview
Dol-Gleizes, F., et al. 2013. Plos One. 8, e80027.
Herbert, C., et al. 2013. Cancer Cell. 23, 489.
Bono. F., et al. 2013. Cancer Cell. 23, 477.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision20-November-2015 JSW
SynonymsFGFR Inhibitor, SSR
DescriptionAn orally bioavailable, highly potent allosteric blocker of multi-fibroblast growth factor receptors (FGFR) that specifically binds to the extracellular domain of the receptor and blocks selective responses mediated by FGFR1-4. Does not compete with FGF for binding to FGFR, but inhibits FGF-induced signaling linked to FGFR internalization. Also, does not show any binding to FGF1 or FGF2. Does not affect the activity of other related receptor tyrosine kinases. Shown to block the FGF2-induced ERK1/2 phosphorylation and prevent translocation of FGFR4 from cell surface to the cytosol, but does not block the phosphorylation of VEGFR2 or MET kinase. Inhibits FGF-1-innduced proliferation of HUVEC (IC50= 100 nM) and hB9-myeloma cells (IC50 = 25 nM) and diminishes FGF-2 induced ERK activation in HEKhFGFR2 WT (IC50 = 28 nM). Also reported to reduce the survival of endothelial cells in a dose-dependent manner (IC50 = 17.7 nM). Suppresses the growth of orthotopic Panc02 and 4T1 xenografts in mice (30 mg/kg/day, p.o) and delays the growth of Lewis lung carcinoma. Also shown to be effective against the multi-drug resistant MCF7/ADR breast cancer xenografts. Synergistically enhances the inhibitory effects of anti-VEGFR2.
FormYellow solid
Intert gas (Yes/No) Packaged under inert gas
CAS number848318-25-2
Chemical formulaC₁₈H₁₅N₂O₄Na
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
-20°C
Hygroscopic
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesDol-Gleizes, F., et al. 2013. Plos One. 8, e80027.
Herbert, C., et al. 2013. Cancer Cell. 23, 489.
Bono. F., et al. 2013. Cancer Cell. 23, 477.