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Telatinib (BAY 57-9352) Chemical Structure
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Biological Activity
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]
References on Telatinib (BAY 57-9352)
- [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
Chemical Information
| Molecular Weight (WM): | 409.83 |
|---|---|
| Formula: | C20H16ClN5O3 |
| CAS No.: | 332012-40-5 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥82mg/mL |
| Water <1mg/mL | |
| Ethanol ≥1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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