| Identification | Back Directory | [Name]
SU5402 | [CAS]
215543-92-3 | [Synonyms]
SU5402
CS-457
CS-1480
PF-02969207
PNU-0290908
SU 5402, >=98%
SU-5402/SU5402
SU5402;SU-5402;SU 5402
SU5402 - CAS 215543-92-3 - Calbiochem
2-[(1,2-Dihydro-2-oxo-3H-indol-3-ylidene)Methyl]-4-Methyl-
3-[3-(2-CARBOXYETHYL)-4-METHYLPYRROL-2-METHYLIDENYL]-2-INDOLINONE
3-[4-METHYL-2-[(2-OXO-1H-INDOL-3-YLIDENE)METHYL]-1H-PYRROL-3-YL]PROPANOIC ACID
2-[(1,2-Dihydro-2-oxo-3H-indol-3-ylidene)methyl]-4-methyl-1H-pyrrole-3-propanoic acid
3-[4-Methyl-2-(2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-1H-pyrrol-3-yl]-propionic acid
1H-Pyrrole-3-propanoic acid, 2-[(1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-4-methyl-
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 | [Molecular Formula]
C17H16N2O3 | [MDL Number]
MFCD08235144 | [MOL File]
215543-92-3.mol | [Molecular Weight]
296.32 |
| Chemical Properties | Back Directory | [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) | [form ]
powder | [pka]
4.60±0.10(Predicted) | [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 |
| Hazard Information | Back Directory | [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. | [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 | [storage]
Store at -20°C | [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 |
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