Size : 25mg
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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.
Cell lines
Human myeloma cell line KMS11
Reaction Conditions
10 μmol/l SU 5402 for 72 h incubation
Applications
The KMS11 human myeloma cell line, which expresses constitutively active mutant FGFR3, displayed an 85% decrease in S-phase cells, a 95% increase in G0/G1 cells, and 4.5-fold increase in apoptotic cells after 72 h treatment with 10 μmol/l SU 5402. Activated extracellular signal-regulated kinases 1 and 2 and signal transducer and activator of transcription 3 were rapidly down-regulated after SU 5402 treatment.
Animal models
BALB/c mice with pre-B-TD cells injected subcutaneously into both flanks
Dosage form
300 ng/kg
Administered by either intraperitoneal injection or direct injection of one of the two tumors
SU 5402 treatment (300 ng/kg) substantially decreased the level of activated ERK1/2 in pre-B-TD cells in vivo.
Note
The technical data provided above is for reference only.
References:
1. Paterson JL, Li Z, Wen XY, et al. Preclinical studies of fibroblast growth factor receptor 3 as a therapeutic target in multiple myeloma. British Journal of Haematology, 2004, 124(5): 595-603.
