Telatinib 化学構造
分子量: 409.83

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製品の説明

生物活性

製品説明 Telatinib は、VEGFR-2、VEGFR-3、c-キットとPGFR-βの強力な阻害剤で、IC50 がそれぞれ 6 nM、4 nM、1 nM 、15 nMです。
ターゲット VEGFR2/3 c-Kit PDGFRα
IC50 6 nM/4 nM 1 nM 15 nM [1]
In vitro試験 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試験 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]
臨床試験 A Phase II study of Telatinib in combination with chemotherapy (Capecitabine and Cisplatin) in subjects with advanced gastric cancer has been completed.
特集

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Telatinib SDF
分子量 409.83
化学式

C20H16ClN5O3

CAS No. 332012-40-5
保管 2年-20℃
6月-80℃in solvent
別名 BAY 57-9352
溶解度 (25°C) * In vitro DMSO 82 mg/mL (200.08 mM)
エタノール 1 mg/mL (2.44 mM)
<1 mg/mL (<1 mM)
* <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.
化学名 4-((4-(4-chlorophenylamino)furo[2,3-d]pyridazin-7-yloxy)methyl)-N-methylpicolinamide

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Source Biochem Pharmacol, 2014, 89(1), 52-61. Telatinib purchased from Selleck
Method ABCG2 ATPase assay
Cell Lines Membranes of high five insect cells overexpressing ABCG2
Concentrations
Incubation Time 15 min
Results Telatinb stimulates the ATPase activity of ABCG2.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description
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