Telatinib

製品コードS2231 バッチS223102

印刷

化学情報

Chemical Structure Synonyms BAY 57-9352 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H16ClN5O3
分子量 409.83 CAS No. 332012-40-5
Solubility (25°C)* 体外 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.

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生物活性

製品説明 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.
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]

プロトコル(参考用のみ)

カスタマーフィードバック

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

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

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。