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Telatinib

Catalog No. T6166 CAS 332012-40-5

Synonyms: Bay 57-9352

Telatinib (Bay 57-9352) is an effective inhibitor of VEGFR2/3, c-Kit, and PDGFRα. The IC50s of Telatinib forVEGFR2/3, c-Kit and PDGFRα are 6 nM/4 nM, 1 nM, and 15 nM, respectively.

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Telatinib, CAS 332012-40-5

Pack Size	Availability	Price/USD
5 mg	In stock	$ 39.00
10 mg	In stock	$ 55.00
25 mg	In stock	$ 122.00
50 mg	In stock	$ 197.00
100 mg	In stock	$ 368.00
1 mL * 10 mM (in DMSO)	In stock	$ 43.00

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Purity: 99.81%

Purity: 98.95%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Telatinib (Bay 57-9352) is an effective inhibitor of VEGFR2/3, c-Kit, and PDGFRα. The IC50s of Telatinib forVEGFR2/3, c-Kit and PDGFRα are 6 nM/4 nM, 1 nM, and 15 nM, respectively.
Targets&IC50	c-Kit:1 nM, PDGFRα:15 nM, VEGFR3:4 nM, VEGFR2:6 nM
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. [3] 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. [4]
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. [1] 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. [2]

Synonyms	Bay 57-9352
Molecular Weight	409.83
Formula	C20H16ClN5O3
CAS No.	332012-40-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 1 mg/mL (2.44 mM)

DMSO: 76 mg/mL (185.4 mM)

References and Literature

1. Steeghs N, et al. Clin Cancer Res, 2008, 14(11), 3470-3476. 2. Strumberg D, et al. Br J Cancer, 2008, 99(10), 1579-1585. 3. Eskens FA, et al. J Clin Oncol, 2009, 27(25), 4169-4176. 4. Langenberg MH, et al. Clin Cancer Res, 2010, 16(7), 2187-2197.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Inhibitor Library Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Compound Library Angiogenesis related Compound Library Anti-Cardiovascular Disease Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Telatinib 332012-40-5 Angiogenesis Tyrosine Kinase/Adaptors c-Kit PDGFR VEGFR CD117 Inhibitor Bay 57-9352 Platelet-derived growth factor receptor inhibit Vascular endothelial growth factor receptor SCFR inhibitor

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