Telatinib (BAY 57-9352) is an orally available, small-molecule inhibitor of vascular endothelial growth factor receptors 2 and 3 (VEGFR-2/-3) and platelet-derived growth factor receptor β tyrosine kinases. Telatinib inhibits VEGFR2 autophosphorylation in a whole-cell assay with an IC50 of 19 nM. Telatinib (BAY 57-9352) blocks PDGF-stimulated growth of human aortic smooth muscle cells with an IC50 of 249 nM. Telatinib treatment significantly inhibits tumor growth and metastasis by blocking the VEGFR signaling and subsequently tumor angiogenesis. 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, DLD-1 colon cancer and H460 non-small cell lung cancer.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 80 mg/mL|
Phase I study of telatinib (BAY 57-9352): analysis of safety, pharmacokinetics, tumor efficacy, and biomarkers in patients with colorectal cancer.
Mross K, et al. Vasc Cell. 2011 Jul 29;3:16. PMID: 21801343.
Phase I evaluation of telatinib, a vascular endothelial growth factor receptor tyrosine kinase inhibitor, in combination with irinotecan and capecitabine in patients with advanced solid tumors.
Langenberg MH, et al. Clin Cancer Res. 2010 Apr 1;16(7):2187-97. PMID: 20233884.
Pharmacogenetics of telatinib, a VEGFR-2 and VEGFR-3 tyrosine kinase inhibitor, used in patients with solid tumors.
Steeghs N, et al. Invest New Drugs. 2011 Feb;29(1):137-43. PMID: 19924384.
|Related VEGFR/PDGFR Products|
SU 5205 is a VEGFR2 inhibitor.
SU-5408 is a potent, cell-permeable inhibitor of mouse VEGFR2 kinase with IC50 of 70 nM.
BFH772 is a potent and selective VEGFR2 inhibitor with an IC50 value of 3 nM.
Ranibizumab is a monoclonal antibody that inhibits angiogenesis by inhibiting Vascular endothelial growth factor A.
NVP-ACC789 is an inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3 and PDGFR-β with IC50s of 0.38, 0.02 (0.23), 0.18, 1.4 μM, respectively.
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