Telatinib|332012-40-5|(替拉替尼; Bay 57-9352)-陌孚医药/Medlife

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Telatinib (Synonyms: 替拉替尼; Bay 57-9352)

目录号: PL09016 纯度: ≥99%

CAS No. :332012-40-5

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中文名称	Telatinib
中文别名	Telatinib(BAY57-9352) 抑制剂;替拉替尼
英文名称	Telatinib
英文别名	2-Pyridinecarboxamide,4-[[[4-[(4-chlorophenyl)amino]furo[2,3-d]pyridazin-7-yl]oxy]methyl]-N-methyl-;Telatinib;2-Pyridinecarboxamide,4-[[[4-[(4-chlorophenyl)amino]furo[2,3-d]pyridazin-7-yl]oxy]methyl]-N-me...;4-[[4-(4-Chloroanilino)furo[2,3-d]pyridazin-7-yl]oxymethyl]-N-methyl-pyridine-2-carboxamide;4-[[4-(4-chloroanilino)furo[2,3-d]pyridazin-7-yl]oxymethyl]-N-methylpyridine-2-carboxamide;Bay 57-9352;Telatinib (BAY 57-9352);4-((4-(4-chlorophenylamino)furo[2,3-d]pyridazin-7-yloxy)methyl)-N-methylpicolinamide;4-(4-(4-chloro-phenylamino)-furo[2,3-d]pyridazin-7-yloxymethyl)-pyridine-2-carboxylic acid methylamide;4-(4-chlorophenylamino)-7-(2-methylaminocarbonyl-4-pyridylmethoxy)furo-[2,3-d]pyridazine;4-[({4-[(4-chlorophenyl)amino]furo[2,3-d]pyridazin-7-yl}oxy)methyl]-N-methyl-2-pyridinecarboxamide;Telatinib,BAY 57-9352,BAY 57-9352;4-[[[4-[(4-Chlorophenyl)amino]furo[2,3-d]pyridazin-7-yl]oxy]methyl]-N-methyl-2-pyridinecarboxamide
Cas No.	332012-40-5
分子式	C₂₀H₁₆N₅O₃Cl
分子量	409.83
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Telatinib是有口服活性的VEGFR2，VEGFR3，PDGFα 和 c-Kit的小分子抑制剂，IC₅₀值分别为6，4，15，1 nM。

生物活性

Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit with IC 50 s of 6, 4, 15 and 1 nM, respectively.

性状

Solid

IC50 & Target[1][2]

VEGFR2 6 nM (IC50) VEGFR3 4 nM (IC50

体外研究(In Vitro)

Telatinib has low affinity for the Raf kinase pathway, epidermal growth factor receptor family, the fibroblast growth factor receptor (FGFR) family, or the Tie-2 receptor. Telatinib is metabolized by various cytochrome P450 (CYP) isoforms including CYP3A4/3A5, CYP2C8, CYP2C9, and CYP2C19 as well as by uridine diphosphate glucuronosyltransferase 1A4 (UGT1A4), with the formation of the N-glucuronides of telatinib as the major biotransformation pathway in man. In vitro studies show telatinib to be a weak substrate of the adenosine triphosphate binding cassette (ABC) B1 (ABCB1) transporter. Telatinib at 1 μM significantly enhances the intracellular accumulation of [H]-mitoxantrone (MX) in ABCG2-overexpressing cell lines. In addition, telatinib at 1 μM significantly reduces the rate of [H]-MX efflux from ABCG2-overexpressing cells. Furthermore, telatinib significantly inhibi

体内研究(In Vivo)

Telatinib causes a significant decrease in endothelium-dependent and endothelium-independent vasodilation. VEGF inhibition by itself decreases NO synthesis, which promotes vasoconstriction, increases peripheral resistance, and therefore can induce an increase in blood pressure. Telatinib (15 mg/kg) with doxorubicin (1.8 mg/kg) significantly decreases the growth rate and tumor size of ABCG2 overexpressing tumors in a xenograft nude mouse model. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Steeghs N, et al. Hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor. Clin Cancer Res. 2008 Jun 1;14(11):3470-6.
[2]. Langenberg MH, et al. Phase I evaluation of telatinib, a vascular endothelial growth factor receptor tyrosine kinase inhibitor, in combination with irinotecan and capecitabine in patients with advanced solid tumors. Clin Cancer Res. 2010 Apr 1;16(7):2187-97.

溶解度数据	In Vitro: DMSO : ≥ 46 mg/mL (112.24 mM)配制储备液

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2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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