1. Protein Tyrosine Kinase/RTK
  2. VEGFR c-Kit PDGFR
  3. 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).

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Henatinib Chemical Structure

Henatinib Chemical Structure

CAS No. : 1239269-51-2

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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].

IC50 & Target

VEGFR-2

0.6 nM (IC50)

PDGFRα

 

PDGFRβ

 

In Vitro

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.

Clinical Trial
Molecular Weight

468.52

Formula

C25H29FN4O4

CAS No.
SMILES

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

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Room temperature in continental US; may vary elsewhere.

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HY-13645
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