1239269-52-3
Chemical Structure
Henatinib maleate
- CAS No.: 1239269-52-3
- Formula:C29H33FN4O8
- Molecular Weight:584.59
IUPAC Name: (R,Z)-2-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-5-(2-hydroxy-3-morpholinopropyl)-3-methyl-5,6,7,8-tetrahydropyrrolo[3,2-c]azepin-4(1H)-one maleate
InChIKey: UGVGACHPGHZDMO-LMERLFCISA-N
SMILES: OC(/C=C\C(O)=O)=O.O=C(/C(C1=C2)=C\C3=C(C4=C(CCCN(C4=O)C[C@H](O)CN5CCOCC5)N3)C)NC1=CC=C2F
Biological Activity: Henatinib maleate is an orally active small-molecule multikinase inhibitor that has demonstrated broad and potent antitumor activities. Henatinib maleate 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 maleate significantly inhibits VEGFR-2 phosphorylation and its downstream signal pathway[1][2].
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Henatinib maleate | Henatinib maleate is an orally active small-molecule multikinase inhibitor that has demonstrated broad and potent antitumor activities. Henatinib maleate 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 maleate significantly inhibits VEGFR-2 phosphorylation and its downstream signal pathway. | |||||||||||||||||||||
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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. [Content Brief]
- [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.
