Telatinib

SKU: orb1301018

Description

Telatinib (Bay 57-9352) is a potent small molecule inhibitor targeting VEGFR2/3, c-Kit, and PDGFRα with IC50 values of 6 nM/4 nM, 1 nM, and 15 nM, respectively. It is widely used in preclinical research for studying angiogenesis and tumor growth in both cellular assays and animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 332012-40-5
• MW: 409.83
• Purity: 98.95%
• Formula: C₂₀H₁₆ClN₅O₃
• SMILES: CNC(=O)c1cc(COc2nnc(Nc3ccc(Cl)cc3)c3ccoc23)ccn1
• Target: VEGFR,PDGFR,c-Kit
• Solubility: 10% DMSO+90% Corn Oil:3.3 mg/mL (8.05 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:1 mg/mL (2.44 mM);DMSO:76 mg/mL (185.44 mM)

Bioactivity

• Target IC50:
  VEGFR2:6 nM|VEGFR3:4 nM|c-Kit:1 nM|PDGFRα:15 nM
• In Vivo:
  Given that tumor development and metastasis are ascribed to deregulated VEGFR signal pathway, Telatinib treatment significantly inhibits tumor growth and metastasis by blocking the VEGFR signaling and subsequently tumor angiogenesis. In addition to the significant inhibition of tumor angiogenesis, Telatinib treatment induces a significant decrease in endothelium-dependent and endothelium-independent vasodilation, as well as reduction in capillary density, leading to an increase in systolic and diastolic blood pressure. 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, Colo-205 colon cancer, DLD-1 colon cancer, and H460 non-small cell lung cancer, as well as pancreatic and prostate carcinoma in a dose-dependent manner.
• In Vitro:
  Telatinib has 0.66, 0.17, and 2.5 times higher IC50 values for VEGFR3, c-Kit, and PDGFRβ than VEGFR2, respectively, while Vatalanib exhibits 18, 20, and 16 times higher IC50 values, respectively, indicating that Telatinib has potential benefit over Vatalanib. Telatinib inhibits VEGFR2 autophosphorylation in a whole-cell assay with an IC50 of 19 nM, suppresses VEGF-dependent proliferation of human umbilical vein endothelial cells with an IC50 of 26 nM, and blocks PDGF-stimulated growth of human aortic smooth muscle cells with an IC50 of 249 nM. Telatinib displays little inhibitory activity against the Raf kinase pathway, epidermal growth factor receptor family, the fibroblast growth factor receptor (FGFR) family, and the Tie-2 receptor.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SCFR, Telatinib, PDGFR, PDGFRα, Vascular endothelial growth factor receptor, VEGFR, VEGFR3, VEGFR2, inhibit, Platelet-derived growth factor receptor, Inhibitor, Bay 57-9352, c-Kit, cKit, CD117

Compound Identifiers

PubChem CID

9808844