Henatinib

Names

[ Name ]:
Henatinib

[Synonym ]:
(R,Z)-2-(5-fluoro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-5-(2-hydroxy-3-morpholin-4-ylpropyl)-3-methyl-5,6,7,8-tetrahydro-1H-pyrrolo[3,2-c]azepin-4-one
UNII-TE20GB753F
Pyrrolo(3,2-c)azepin-4(1H)-one,2-((Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-5,6,7,8-tetrahydro-5-((2R)-2-hydroxy-3-(4-morpholinyl)propyl)-3-methyl
Henatinib

Biological Activity

[Description]:

Henatinib is an orally active small-molecule multikinase inhibitor that has demonstrated broad and potent antitumor activities. Henatinib inhibits the activity of VEGFR-2, c-kit, PDGFR with IC50 values of 0.6 nM, 3.3 nM and 41.5 nM, respectively. Henatinib significantly inhibits VEGFR-2 phosphorylation and its downstream signal pathway in human umbilical vein endothelial cells (HUVECs)[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit

[Target]

VEGFR-2:0.6 nM (IC50)

PDGFRα

PDGFRβ

[In Vitro]

Henatinib shows high binding affinities for VEGFRs, PDGFR and stem cell factor receptor[1]. Henatinib significantly inhibits VEGFR-2 phosphorylation and its downstream signal pathway in human umbilical vein endothelial cells (HUVECs), and consistently inhibited VEGF-stimulated HUVEC proliferation, migration and tubule formation[2].

[References]

[1]. Jun Qian, et al. Determination of henatinib in human plasma and urine by liquid chromatography-tandem mass spectrometry and its pharmacokinetic application. J Pharm Biomed Anal. 2013 Jun;80:173-9.

[2]. Haitian Quan, et al. Abstract 4259: Preclinical anti-tumor study of henatinib, a novel and selective inhibitor of VEGFR-2 in phase I clinical trials. Cancer Res (2011) 71 (8_Supplement): 4259.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₂₉FN₄O₄

[ Molecular Weight ]:
468.52100

[ Exact Mass ]:
468.21700

[ PSA ]:
101.39000

[ LogP ]:
1.99730

Related Compounds

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