| Identification | Back Directory | [Name]
Henatinib | [CAS]
1239269-51-2 | [Synonyms]
Henatinib
2-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-5-[(2R)-2-hydroxy-3-morpholin-4-ylpropyl]-3-methyl-1,6,7,8-tetrahydropyrrolo[3,2-c]azepin-4-one
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- | [Molecular Formula]
C25H29FN4O4 | [MOL File]
1239269-51-2.mol | [Molecular Weight]
468.52 |
| Hazard Information | Back Directory | [Uses]
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]. | [IC 50]
VEGFR-2: 0.6 nM (IC50); PDGFRα; PDGFRβ | [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. DOI:10.1016/j.jpba.2013.03.010
[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. |
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