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Cat. No. Name Size Price Add Cart
KI3305SU 5402QuoteQuote

Chemical Characteristic

Product NameSU 5402
CAS No.215543-92-3
Molecular Weight 296.32
FormulaC17H16N2O3
Chemical Name3-(4-methyl-2-((2-oxoindolin-3-ylidene)methyl)-1H-pyrrol-3-yl)propanoic acid
SmilesC(=O)(CCc1c([nH]cc1C)/C=C/1\C(=O)Nc2c1cccc2)O
Chemical Structure

Biological activities

SU5402 is a potent and selective inhibitor of vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR). The IC50s of SU5402 against VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rβ tyrosine kinases are 20, 30, and 510 nM, respectively. SU5402 is less potent to inhibit the activity of EGFR with an IC50 of > 100 µM.[1] SU5402 specifically inhibits the growth of the two t(4;14)-positive multiple myeloma (MM) lines, KMS-11 and OPM-2.[2] In vitro, SU5402 treatment (10 µM) causes an 85% decrease in S-phase cells, a 95% increase in G0/G1 cells, and 4.5-fold increase in apoptotic cells of the KMS11 human myeloma cell line, which expresses constitutively active mutant FGFR3. SU5402 treatment rapidly decreases activated extracellular signal-regulated kinases 1 and 2 (ERK1/2) and signal transducer and activator of transcription 3 (Stat3) in vitro. SU5402 treatment also abrogates the stimulating effect of aFGF ligand in human myeloma cell lines expressing wild-type FGFR3. In addition, SU5402 inhibits FGFR3 phosphorylation in vitro and in murine MM tumor models.[3]

Protocols

In vitro: SU5402 is dissolved in DMSO.[4]

References

[1] Sun L, et al. Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases. J Med Chem. 1999, 42(25): 5120-5130.
[2] Grand EK, et al. Targeting FGFR3 in multiple myeloma: inhibition of t(4;14)-positive cells by SU5402 and PD173074. Leukemia. 2004, 18(5): 962-966.
[3] Paterson JL, et al. Preclinical studies of fibroblast growth factor receptor 3 as a therapeutic target in multiple myeloma. Br J Haematol. 2004, 124(5): 595-603.
[4] Terry J, et al. Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin prevents synovial sarcoma proliferation via apoptosis in in vitro models. Clin Cancer Res. 2005, 11(15): 5631-5638.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

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