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Alvespimycin
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。
Alvespimycin图片
CAS NO:467214-20-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
阿螺旋霉素
17-DMAG
NSC 707545
产品介绍
Alvespimycin (17-DMAG) 是一种有效的Hsp90抑制剂,结合到 Hsp90,EC50为 62 ± 29 nM。
生物活性

Alvespimycin (17-DMAG) is a potent inhibitor ofHsp90, binding toHsp90with anEC50of 62 ± 29 nM.

IC50& Target

HSP90

62 nM (EC50)

GRP94

65 nM (EC50)

体外研究
(In Vitro)

Alvespimycin (17-DMAG) is a potent inhibitor of Hsp90, binding to Hsp90 with an EC50of 62 nM. Alvespimycin (17-DMAG) inhibits the growth of the human cancer cell lines SKBR3 and SKOV3, which overexpress Hsp90 client protein Her2, and causes down-regulation of Her2 as well as induction of Hsp70 consistent with Hsp90 inhibition, for Her2 degradation with EC50of 8 ± 4 nM and 46 ± 24 nM in SKBR3 and SKOV3 cells, respectively; for Hsp70 induction with EC50of 4 ± 2 nM and 14 ± 7 nM in SKBR3 and SKOV3 cells, respectively[1]. Compared with the vehicle control, Alvespimycin (17-DMAG) dose-dependent apoptosis (P<0.001 averaged across 24- and 48-hour time points) at concentrations of 50 nM to 500 nM, which represent pharmacologically attainable doses. Similar to many other agents, Alvespimycin (17-DMAG) also demonstrates time-dependent apoptosis (P<0.001, averaged across all doses) in chronic lymphocytic leukemia (CLL) cells with extended exposure from 24 to 48 hours. In addition,Alvespimycin (17-DMAG) is much more potent after 24 and 48 hours of treatment than 17-AAG[2].

体内研究
(In Vivo)

The tumors are grown for two months before the start of i.p. injections every four days over one month with 0, 50, 100 and 200 mg/kg dipalmitoyl-radicicol or 0, 5, 10 and 20 mg/kg Alvespimycin (17-DMAG). Despite sample heterogeneity, the HSP90 inhibitor-treated animals have significantly lower tumour volumes than the vehicle control-treated animals. HSP90 inhibitors have been shown to cause liver toxicity in an animal model of gastrointestinal cancer. Nevertheless, the reduction in tumor size using dipalmitoyl-radicicol is statistically significant at 100 mg/kg, while Alvespimycin (17-DMAG) at either 10 or 20 mg/kg elicits a significant reduction in tumor size[3].

Clinical Trial
分子量

616.75

Formula

C32H48N4O8

CAS 号

467214-20-6

中文名称

阿螺旋霉素

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.