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Henatinib

CAT: 0804-HY-13645Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-13645Size:1 Each
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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