Telatinib 332012-40-5

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Molecular Weight:

409.83 Telatinib is a Potent Inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively. Phase 2.


Biological Activity


Telatinib has 0.66, 0.17, and 2.5 times higher IC50 values for VEGFR3,
c-Kit, and PDGFRβ than VEGFR2, respectively, while Vatalanib exhibits
18, 20, and 16 times higher IC50 values, respectively, indicating that
Telatinib has potential benefit over Vatalanib. Telatinib inhibits
VEGFR2 autophosphorylation in a whole-cell assay with an IC50 of 19 nM,
suppresses VEGF-dependent proliferation of human umbilical vein
endothelial cells with an IC50 of 26 nM, and blocks PDGF-stimulated
growth of human aortic smooth muscle cells with an IC50 of 249 nM. Telatinib displays little inhibitory activity against the Raf kinase
pathway, epidermal growth factor receptor family, the fibroblast growth
factor receptor (FGFR) family, and the Tie-2 receptor.


Given that tumor development and metastasis are ascribed to deregulated
VEGFR signal pathway, Telatinib treatment significantly inhibits tumor
growth and metastasis by blocking the VEGFR signaling and subsequently
tumor Angiogenesis. In addition to the significant inhibition of tumor
angiogenesis, Telatinib treatment induces a significant decrease in
endothelium-dependent and endothelium-independent vasodilation, as well
as reduction in capillary density, leading to an increase in systolic
and diastolic blood pressure. Administration of Telatinib
as a single agent exhibits a potent anti-tumor activity in multiple
human tumor xenograft models including MDA-MB-231 breast cancer,
Colo-205 colon cancer, DLD-1 colon cancer, and H460 non-small cell lung
cancer, as well as pancreatic and prostate carcinoma in a dose-dependent
manner.

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Product Categories : Protein Tyrosine Kinase > VEGFR Inhibitor