Telatinib mesylate Bay 57-9352 mesylate|cas:332013-26-0|西域试剂

Telatinib mesylate Bay 57-9352 mesylate,99.46%

产品编号：Bellancom-10527C| CAS NO：332013-26-0| 分子式：C₂₁H₂₀ClN₅O₆S| 分子量：505.93

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-10527C	￥800.00	杭州北京（现货）
Bellancom-10527C	￥1200.00	杭州北京（现货）
Bellancom-10527C	￥2400.00	杭州北京（现货）
Bellancom-10527C	￥3600.00	杭州北京（现货）
Bellancom-10527C	￥5000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Telatinib mesylate Bay 57-9352 mesylate

产品介绍

Telatinib mesylate (Bay 57-9352 mesylate) 是一种有效的的口服活性的 VEGFR2，VEGFR3，PDGFα 和 c-Kit 抑制剂，IC₅₀ 分别为 6 nM，4 nM，15 nM 和 1 nM。

生物活性

Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC₅₀s of 6 nM, 4 nM, 15 nM and 1 nM, respectively.

体外研究

Telatinib enhances the anticancer activity of ABCG2 substrate anticancer drugs by inhibiting ATP-binding cassette G2 (ABCG2) efflux transporter activity. Co-incubation of ABCG2-overexpressing drug resistant cell lines with Telatinib and ABCG2 substrate anticancer drugs significantly reduces cellular viability, whereas Telatinib alone does not significantly affect drug sensitive and drug resistant cell lines. Telatinib at 1 μM does not significantly alter the expression of ABCG2 in ABCG2-overexpressing cell lines. Telatinib at 1 μM significantly enhances the intracellular accumulation of [³H]-mitoxantrone (MX) in ABCG2-overexpressing cell lines.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Telatinib (15 mg/kg; oral dministration; every 2nd and 3rd day; total 12 times; male athymic NCR (nu/nu) nude mice) with Doxorubicin (1.8 mg/kg) significantly decreases the growth rate and tumor size of ABCG2 overexpressing tumors in a xenograft nude mouse model.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male athymic NCR (nu/nu) nude mice (13-15 g, age 4-5 weeks) injected with H460 and H460/MX20 cells
Dosage:	15 mg/kg
Administration:	Oral dministration; every 2nd and 3rd day; total 12 times
Result:	With Doxorubicin (1.8 mg/kg) significantly decreased the growth rate and tumor size of ABCG2 overexpressing tumors in a xenograft nude mouse model.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male athymic NCR (nu/nu) nude mice (13-15 g, age 4-5 weeks) injected with H460 and H460/MX20 cells
Dosage:	15 mg/kg
Administration:	Oral dministration; every 2nd and 3rd day; total 12 times
Result:	With Doxorubicin (1.8 mg/kg) significantly decreased the growth rate and tumor size of ABCG2 overexpressing tumors in a xenograft nude mouse model.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (494.14 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9766 mL	9.8828 mL	19.7656 mL
5 mM	0.3953 mL	1.9766 mL	3.9531 mL
10 mM	0.1977 mL	0.9883 mL	1.9766 mL

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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献