3-[2,4-dimethyl-5-[(E)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid

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Product Name	3-[2,4-dimethyl-5-[(E)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
CAS No	252916-29-3
EC-No
Min. Order	1G
Purity	99%
Supply Ability	100KG
Release date	2019/07/06

AD68

3-[2,4-dimethyl-5-[(E)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid Basic information

Product Name:	3-[2,4-dimethyl-5-[(E)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
Synonyms:	3-[2,4-dimethyl-5-[(E)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid;TSU-68;5-[1,2-Dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-propanoic acid;(Z)-3-(2,4-dimethyl-5-((2-oxoindolin-3-ylidene)methyl)-1H-pyrrol-3-yl)propanoic acid;TSU-68 (SU6668);1H-Pyrrole-3-propanoic acid, 5-[(1,2-dihydro-2-oxo-3H-indol-3-ylidene)Methyl]-2,4-diMethyl-;SU 6668(TSU-68);(E)-3-(2,4-diMethyl-5-((2-oxoindolin-3-ylidene)Methyl)-1H-pyrrol-3-yl)propanoic acid
CAS:	252916-29-3
MF:	C18H18N2O3
MW:	310.36
EINECS:
Product Categories:	Angiogenesis and Metastasis;API;Inhibitors
Mol File:	252916-29-3.mol

3-[2,4-dimethyl-5-[(E)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid Chemical Properties

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3-[2,4-dimethyl-5-[(E)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid Usage And Synthesis

Uses	TSU-68 (SU6668, Orantinib) is a potent inhibitor of Flk-1/KDR, FGFR1 and PDGFRβ with Ki of 2.1 μM, 1.2 μM, and 8 nM, respectively.
Uses	TSU-68 is a inhibitor that targets vascular endothelial growth factor receptor 2, platelet-derived growth factor receptor β, and fibroblast growth factor receptor 1. The inhibitory effects of TSU-68 t owards these growth factors lead to substantial antitumor activity and showed potential in its development in therapeutic uses.
Definition	ChEBI: An oxindole that is 3-methyleneoxindole in which one of the hydrogens of the methylene group is substituted by a 2-(2-carboxyethyl)-3,5-dimethylpyrrol-3-yl group. It is an ATP-competitive inhibitor of the tyrosine kinase activity of fibroblast growth facto receptor 1.
Biological Activity	ATP-competitive PDGFR, VEGF and FGFR inhibitor (IC 50 values are 0.06, 2.43, 3.04 and > 100 μ M at PDGFR β , VEGFR2, FGFR1 and EGFR respectively). Inhibits proliferation of HUVEC and NIH3T3 cells in vitro (IC 50 values are 0.41, 9.3 and 16.5 μ M for VEGF, FGF and PDGF-stimulated growth respectively) and induces > 75% growth inhibition against a broad range of tumor types in vivo . Exhibits antiangiogenic, anti-inflammatory, antimetastatic and proapoptotic activity and is orally active.

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