上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
Telatinib (Synonyms: Bay 57-9352) 纯度: 98.72%
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。
Telatinib Chemical Structure
CAS No. : 332012-40-5
规格 | 价格 | 是否有货 | 数量 |
---|---|---|---|
10 mM * 1 mL in DMSO | ¥880 | In-stock | |
5 mg | ¥800 | In-stock | |
10 mg | ¥1200 | In-stock | |
25 mg | ¥2400 | In-stock | |
50 mg | ¥3600 | In-stock | |
100 mg | ¥5000 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
* Please select Quantity before adding items.
Telatinib 相关产品
•相关化合物库:
- Drug Repurposing Compound Library Plus
- Clinical Compound Library Plus
- Bioactive Compound Library Plus
- Kinase Inhibitor Library
- Protein Tyrosine Kinase Compound Library
- Anti-Cancer Compound Library
- Clinical Compound Library
- Drug Repurposing Compound Library
- Differentiation Inducing Compound Library
- Reprogramming Compound Library
- Anti-COVID-19 Compound Library
- Orally Active Compound Library
- Anti-Breast Cancer Compound Library
- Anti-Lung Cancer Compound Library
- Anti-Pancreatic Cancer Compound Library
- Anti-Blood Cancer Compound Library
- Angiogenesis Related Compound Library
- Anti-Liver Cancer Compound Library
- Rare Diseases Drug Library
- Anti-Colorectal Cancer Compound Library
生物活性 |
Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit with IC50s of 6, 4, 15 and 1 nM, respectively. |
||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
IC50 & Target |
|
||||||||||||||||
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[2]. 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[3]. Telatinib at 1 μM significantly enhances the intracellular accumulation of [3H]-mitoxantrone (MX) in ABCG2-overexpressing cell lines. In addition, telatinib at 1 μM significantly reduces the rate of [3H]-MX efflux from ABCG2-overexpressing cells. Furthermore, telatinib significantly inhibits ABCG2-mediated transport of [3H]-E217βG in ABCG2 overexpressing membrane vesicles[4]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||||||
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[1]. 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[4]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||||||
Clinical Trial |
|
||||||||||||||||
分子量 |
409.83 |
||||||||||||||||
Formula |
C20H16ClN5O3 |
||||||||||||||||
CAS 号 |
332012-40-5 |
||||||||||||||||
中文名称 |
替拉替尼;特拉替尼 |
||||||||||||||||
运输条件 |
Room temperature in continental US; may vary elsewhere. |
||||||||||||||||
储存方式 |
|
||||||||||||||||
溶解性数据 |
In Vitro:
DMSO : ≥ 46 mg/mL (112.24 mM) * “≥” means soluble, but saturation unknown. 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
||||||||||||||||
参考文献 |
|
Kinase Assay [4] |
The vanadate (Vi)-sensitive ATPase activity of ABCG2 in the membrane of High Five insect cells is measured. Briefly, membrane (2 μg/0.06 mL) are incubated in ATPase assay buffer with or without 0.4 mM vanadate at 37°C for 5 min and then incubated with varying concentrations of telatinib at 37°C for 5 min. The ATPase reaction is started by the addition of 4 mM Mg-ATP. After incubating at 37°C for 10 min, the reactions are stopped by adding 0.05 mL of 10% SDS solution. The liberated inorganic phosphate is measured[4]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
---|---|
Animal Administration [4] |
Mice: The mice are randomized into four groups and treated with one of the following regimens: (a) vehicle (10% N-methyl-pyrrolidinone, 90% polyethylene glycol 300) (q3d×6), (b) DOX (1.8 mg/kg, i.p., q3d×6), (c) telatinib dissolved in 10% N-methyl-pyrrolidinone, 90% polyethylene glycol 300 (15 mg/kg, p.o., every 2nd and 3rd day; total 12 times), and (d) DOX (1.8 mg/kg, i.p., q3d×6) + telatinib (15 mg/kg, p.o., every 2nd and 3rd day, given 1 h before giving DOX; total 12 times). DOX for injection is prepared by dissolving in saline. Tumor volume is measured using calipers and body weights are recorded[4]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
|
所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务