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[1][2].

Product Specifications

CAS Number

[1239269-52-3]

UNSPSC

12352005

Target

C-Kit; PDGFR; VEGFR

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

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

Molecular Formula

C29H33FN4O8

Molecular Weight

584.59

References & Citations

[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.