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SU 5402

Catalog No.
A3843
VEGFR2/FGFR/PDGFR/EGFR inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$77.00
In stock
10mg
$80.00
In stock
25mg
$170.00
In stock
50mg
$310.00
In stock

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Email: [email protected]

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Background

IC50: 0.02, 0.03, 0.51 and > 100 μM for VEGFR2, FGFR1, PDGFRβ and EGFR, respectively

SU 5402 is an inhibitor of VEGF, FGF, and PDGF receptor tyrosine kinases. Receptor tyrosine kinases have been recognized as therapeutic targets for the treatment of human diseases including cancers, inflammatory diseases, and cardiovascular diseases.

In vitro: SU5402 could inhibit FGFR3 phosphorylation in vitro. B cells dependent on FGFR3 for survival were sensitive to SU5402 specifically. A panel of 11 human myeloma cell lines was studied, among which five beared t(4;14) translocation. The KMS11 human myeloma cell line expressesing constitutively active mutant FGFR3, displayed a 95% increase in G0/G1 cells as well as 45-fold increase in apoptotic cells after SU5402 treatment. In addition, the activated signal-regulated kinases 1 and 2 and signal activator of transcription 3 were down-regulated after SU5402 treatment rapidly. In human myeloma cell lines with wild-type FGFR3, the stimulating effect of aFGF ligand was abrogated by SU5402 [1].

In vivo: BALB/c mice were inoculated with syngeneic pre-B-TD cells and these established tumours were treated with 300 ng/kg SU5402 or carrier alone administered by either direct subcutaneous or intraperitoneal injection. Tumours were collected 24 h later and Western blot analyses indicated a treatment-related decrease in the levels of activated ERK1/2 in the harvested tumors [1].

Clinical trial: N/A

Reference:
[1] Paterson JL,Li Z,Wen XY,Masih-Khan E,Chang H,Pollett JB,Trudel S,Stewart AK.  Preclinical studies of fibroblast growth factor receptor 3 as a therapeutic target in multiple myeloma. Br J Haematol.2004 Mar;124(5):595-603.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt296.33
Cas No.215543-92-3
FormulaC17H16N2O3
SynonymsSU-5402; SU5402
Solubility≥14.8 mg/mL in DMSO, insoluble in EtOH,insoluble in H2O
Chemical Name3-[4-methyl-2-[(Z)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
SDFDownload SDF
Canonical SMILESCC1=CNC(=C1CCC(=O)O)C=C2C3=CC=CC=C3NC2=O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Chemical structure

SU 5402