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| Product Name: | SU5402 | | Synonyms: | SU5402;3-[4-METHYL-2-[(2-OXO-1H-INDOL-3-YLIDENE)METHYL]-1H-PYRROL-3-YL]PROPANOIC ACID;3-[3-(2-CARBOXYETHYL)-4-METHYLPYRROL-2-METHYLIDENYL]-2-INDOLINONE;2-[(1,2-Dihydro-2-oxo-3H-indol-3-ylidene)Methyl]-4-Methyl-;SU-5402/SU5402;2-[(1,2-Dihydro-2-oxo-3H-indol-3-ylidene)methyl]-4-methyl-1H-pyrrole-3-propanoic acid
3-[3-(2-Carboxyethyl)-4-methylpyrrol-2-methylidenyl]-2-indolinone;3-[4-Methyl-2-(2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-1H-pyrrol-3-yl]-propionic acid;PF-02969207 | | CAS: | 215543-92-3 | | MF: | C17H16N2O3 | | MW: | 296.32 | | EINECS: | | Product Categories: | Angiogenesis and Metastasis;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals | | Mol File: | 215543-92-3.mol |
| SU5402 Chemical Properties |
| Melting point | >222°C (dec.) | | Boiling point | 592.6±50.0 °C(Predicted) | | density | 1.363±0.06 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | DMSO: soluble10mg/mL (clear solution) | | pka | 4.60±0.10(Predicted) | | form | powder | | color | light orange to dark orange | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. | | InChIKey | JNDVEAXZWJIOKB-JYRVWZFOSA-N |
| SU5402 Usage And Synthesis |
| Description | SU-5402 (215543-92-3) inhibits FGFR phosphorylation in vitro, in cell culture1, and in mouse tumor cell models2. SU-5402 can suppress ECP induced cardiomyocyte differentiation of P19CL6 embryonic carcinoma cells via an FGFR3 dependent pathway.3 | | Chemical Properties | Yellow-Green Solid | | Uses | A specific FGFR (fibroblast growth factor receptor
er. | | Uses | SU 5402 is a specific FGFR (fibroblast growth factor receptor) inhibitor (1,2,3,4). It is also an intermediate for 3-(hetero)arylmethylidene-2-indolinone derivatives as modulators of protein kinase activity for use in treating cancer. | | Uses | SU5402 has been used as a fibroblast growth factor receptor inhibitor:- in cell signalling experiments to stimulate cells for MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay
- to study its effect on the expression of osteogenic markers and expression of osteoprotegerin and RANKL (runt-related transcription factor(RUNX)-2
- to prepare a stock solution with DMSO (Dimethyl superoxide) for cell culture medium and also to co-treat embryos
- to study its effect on osteogenic markers.
| | Definition | ChEBI: An oxindole that is 3-methyleneoxindole in which one of the hydrogens of the methylene group is substituted by a 3-(2-carboxyethyl)-4-methyl-1H-pyrrol-2-yl group. It is an ATP-competitive inhibitor of the tyrosine kinase activity of fibr
blast growth factor receptor 1. | | Biological Activity | Potent and selective vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) inhibitor (IC 50 values are 0.02, 0.03, 0.51 and > 100 μ M at VEGFR2, FGFR1, PDGFR β and EGFR respectively). Inhibits embryonic left-right determination and exhibits potent anticancer activity in vitro and in vivo . | | Biochem/physiol Actions | SU-5402 has inhibitory effect on the action of tyrosine kinases. It competitively binds to the ATP-binding site on the fibroblast growth factor receptor (FGFR). | | 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]. | | IC 50 | 0.02, 0.03, 0.51 and > 100 μm for vegfr2, fgfr1, pdgfrβ and egfr, respectively | | References | 1) Lee et al. (2013), Interleukin-1β enhances cell migration through AP-κ1 and NF-B pathway dependent FGF2 expression in human corneal endothelial cells; Biol. Cell, 105 175
2) Paterson et al. (2004), Preclinical studies of fibroblast growth factor receptor 3 as a therapeutic target in multiple myeloma; Br. J. Haematol., 124 595
3) Jin et al. (2012), Eosinophil cationic protein enhances cardiomyocyte differentiation of P19CL6 embryonal carcinoma cells by stimulating the FGF receptor signaling pathway; Growth Factors, 30 344 |
| SU5402 Preparation Products And Raw materials |
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