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Telatinib mesylate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Telatinib mesylate图片
CAS NO:332013-26-0
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
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VEGFR2VEGFR3PDGFαc-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 activeVEGFR2,VEGFR3,PDGFα, andc-Kitinhibitor withIC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively[1].

IC50& Target[1]

VEGFR2

6 nM (IC50)

VEGFR3

4 nM (IC50)

PDGFRα

15 nM (IC50)

c-Kit

1 nM (IC50)

体外研究
(In Vitro)

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[2].
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[2].

体内研究
(In Vivo)

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[2].

Animal Model:Male athymic NCR (nu/nu) nude mice (13-15 g, age 4-5 weeks) injected with H460 and H460/MX20 cells[2]
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.
Clinical Trial
分子量

505.93

性状

Solid

Formula

C21H20ClN5O6S

CAS 号

332013-26-0

中文名称

甲磺酸替拉替尼;甲磺酸特拉替尼

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)

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 mg5 mg10 mg
1 mM1.9766 mL9.8828 mL19.7656 mL
5 mM0.3953 mL1.9766 mL3.9531 mL
10 mM0.1977 mL0.9883 mL1.9766 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。