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Novel Inhibitor for Fibroblast Growth Factor Receptor Tyrosine Kinase

Novel Inhibitor for Fibroblast Growth Factor Receptor Tyrosine Kinase

Naparat Kammasud, Chantana Boonyarat, Satoshi Tsunoda, Hiroaki Sakurai, Ikuo Saiki, David S Grierson, Opa Vajragupta

Bioorg Med Chem Lett. 2007 Sep 1;17(17):4812-8.

PMID: 17618113

Abstract:

NP603, the 6-dimethoxy phenyl indolin-2-one, was designed as FGF receptor 1 inhibitor by computational study. NP603 was synthesized and found to be more active against endothelial proliferation of HUVEC after the rhFGF-2 stimulation than SU6668 with minimum effective dose of 0.4 microM but with similar potency as SU16g. NP603 inhibited the tyrosine phosphorylation in FGF receptor and the activation of extracellular signal-regulated kinase and c-Jun-N-terminal-kinase after the rhFGF-2 stimulation. The increase in activity of NP603 supports the role of Lys514 movement in ligand-receptor binding in modeling study as the movement accommodates the hydrophobic interaction at the receptor pocket leading to the enhancement of binding capacity.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP949164801-B	NP603		949164-80-1	Price

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