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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].

Product Specifications

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

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