Henatinib

• 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].

• CAS Number :

  [1239269-51-2]

• UNSPSC :

  12352005

• Target :

  C-Kit; PDGFR; VEGFR

• Type :

  Reference compound

• Related Pathways :

  Protein Tyrosine Kinase/RTK

• Applications :

  Cancer-Kinase/protease

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/henatinib.html

• Solubility :

  10 mM in DMSO

• Smiles :

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

• Molecular Formula :

  C25H29FN4O4

• Molecular Weight :

  468.52

• 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.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 1

• Isoform :

  PDGFRα; PDGFRβ; VEGFR2/KDR/Flk-1