Telatinib

Catalog No.S2231 Batch:S223101

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Technical Data

Formula

C20H16ClN5O3
Molecular Weight 409.83 CAS No. 332012-40-5
Solubility (25°C)* In vitro DMSO 82 mg/mL (200.08 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Telatinib (BAY 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively. Phase 2.
Targets
c-Kit [1] VEGFR3 [1] VEGFR2 [1] PDGFRα [1]
1 nM 4 nM 6 nM 15 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]

Protocol (from reference)

Customer Product Validation

Data from [Biochem Pharmacol, 2014, 89(1), 52-61]

Data from [Data independently produced by , , Clin Cancer Res, 2018, 24(11):2678-2687]

Selleck's Telatinib has been cited by 5 publications

Screening of ETO2-GLIS2-induced Super Enhancers identifies targetable cooperative dependencies in acute megakaryoblastic leukemia [ Sci Adv, 2022, 8(6):eabg9455] PubMed: 35138899
Unravelling vascular tumors: combining molecular and computational biology [ Leiden University Scholarly Publications, 2020, N/A] PubMed: N/A
A Subset of TREM2+ Dermal Macrophages Secretes Oncostatin M to Maintain Hair Follicle Stem Cell Quiescence and Inhibit Hair Growth [ Cell Stem Cell, 2019, 24(4):654-669] PubMed: 30930146
Telatinib Is an Effective Targeted Therapy for Pseudomyogenic Hemangioendothelioma [van IJzendoorn DGP Clin Cancer Res, 2018, 24(11):2678-2687] PubMed: 29511030
Telatinib reverses chemotherapeutic multidrug resistance mediated by ABCG2 efflux transporter in vitro and in vivo. [Sodani K Biochem Pharmacol, 2014, 89(1):52-61] PubMed: 24565910

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.