Telatinib (BAY 57-9352) is a potent inhibitor of VEGFR-2, VEGFR-3, c-Kit and PGFR-β with IC50 of 6 nM, 4 nM, 1 nM and 15 nM, respectively. Telatinib binds to and inhibits the vascular endothelial growth factor receptors (VEGFRs) type 2 and 3, platelet-derived growth factor receptor beta (PDGFRb) and c-Kit, which may result in the inhibition of angiogenesis and cellular proliferation in tumors in which these receptors are upregulated. These telatinib-inhibited receptor protein tyrosine kinases are overexpressed or mutated in many tumor cell types and may play key roles in tumor angiogenesis and tumor cell proliferation. 17-AAG is a synthetic analogue of the benzoquinone ansamycin antibiotic geldanamycin and has also been found to inhibit the molecular chaperone Hsp90.  ^[1][2]

 

 

 

 

[1] Clin. Cancer Res. 2008, 14, 3470-3476.

[2] Br. J Cancer 2008, 99, 1579-1585.