Skip to Content
Merck

5.33434

FGFR Inhibitor, SSR128129E

Synonym(s):

FGFR Inhibitor, SSR128129E, FGFR Inhibitor, SSR

Sign In to View Organizational & Contract Pricing.

Select a Size

About This Item

Empirical Formula (Hill Notation):
C18H15N2NaO4
CAS Number:
848318-25-2
Molecular Weight:
346.31
MDL number:
MFCD25976751
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

View All Documentation
Technical Service
Need help? Our team of experienced scientists is here for you.
Let Us Assist
Technical Service
Need help? Our team of experienced scientists is here for you.
Let Us Assist

SMILES string

[Na+].[n]21c(c(c(c2C(=O)c3cc(c(cc3)N)C(=O)[O-])C)OC)cccc1

InChI

1S/C18H16N2O4.Na/c1-10-15(20-8-4-3-5-14(20)17(10)24-2)16(21)11-6-7-13(19)12(9-11)18(22)23;/h3-9H,19H2,1-2H3,(H,22,23);/q;+1/p-1

InChI key

JFBMSTWZURKQOC-UHFFFAOYSA-M

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

color

yellow

solubility

DMSO: 50 mg/mL

storage temp.

−20°C

Quality Level

100

Related Categories

General description

An 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.
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.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
FGFR

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

Global Trade Item Number

SKUGTIN
5.33434.000104055977286908

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service