Henatinib 

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

468.52

C₂₅H₂₉FN₄O₄

1239269-51-2

O=C1N(C[C@H](O)CN2CCOCC2)CCCC3=C1C(C)=C(/C=C4C(NC5=C\4C=C(F)C=C5)=O)N3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.