United States (Change Country)Telatinib (BAY 57-9352) Chemical Structure
Telatinib (BAY 57-9352) is an orally available, potent multitargeted VEGFR-2, VEGFR-3, PDGFR-β and c-Kit tyrosine kinases inhibitor with an IC50 of 19 nM for the inhibition of VEGFR-2 autophosphorylation. Telatinib (BAY 57-9352, CP 127374; KOS 953; NSC 330507; Tanespimycin) also inhibits VEGF-dependent proliferation of human umbilical vein endothelial cells (HUVECs) with an IC50 of 26 nM and PDGF-stimulated growth of human aortic smooth muscle cells with an IC50 of 249 nM. Telatinib (BAY 57-9352, CP 127374; KOS 953; NSC 330507; Tanespimycin) demonstrates anti-tumor activity in various cancer models. Formation of the N-glucuronides of telatinib is identified as the major biotransformation pathway in man. Telatinib (BAY 57-9352, CP 127374; KOS 953; NSC 330507; Tanespimycin) is metabolized by various CYP isoforms and UGT1A4. [1][2][3]
[1] Clin Cancer Res 2008;14:3470-3476
[2] J Clin Oncol 2009;27:4169-4176
[3] British Journal of Cancer 2008;99:1579 – 1585
| Molecular Weight (WM): | 409.83 |
|---|---|
| Formula: | C20H16ClN5O3 |
| Solubility(R.T.:25°C): | DMSO 82mg/mL |
| Water <1mg/mL | |
| Ethanol 1mg/mL |
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