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Telatinib

Cat. No. M1994
Telatinib Structure
Synonym:

BAY 57-9352

Size Price Availability Quantity
10mg USD 240 In stock
50mg USD 720 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 409.83
Formula C20H16ClN5O3
CAS Number 332012-40-5
Purity >98%
Solubility DMSO 80 mg/mL
Storage at -20°C
References

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.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Telatinib, BAY 57-9352 supplier, VEGFR/PDGFR, inhibitors

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