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Retaspimycin
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。
Retaspimycin图片
CAS NO:857402-23-4
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
瑞他霉素
产品介绍
Retaspimycin 是一种有效的Hsp90抑制剂,对 Hsp90 和 Grp9 的EC50值均为 119 nM。
生物活性

Retaspimycin is a potent inhibitor ofHsp90, withEC50s of 119 nM for bothHsp90and Grp9.

IC50& Target[1]

HSP90

119 nM (EC50)

GRP94

119 nM (EC50)

体外研究
(In Vitro)

Retaspimycin is a potent inhibitor of Hsp90, with EC50s of 119 nM for both Hsp90 and Grp9. Retaspimycin (IPI-504) is cytocoxic to human multiple myeloma (MM) cell lines, with EC50s of 307 ± 51 nM and 306 ± 38 nM, respectively, for MM1.s and RPMI-8226 cells[1]. Retaspimycin (IPI-504, 10-100 nM) suppresses the growth of both trastuzumab-sensitive and -resistant cells in a dose-dependent manner. Retaspimycin (0-500 nM) decreases HER2 protein expression and suppresses both Akt and MAPKs pathways in both sensitive and trastuzumab-resistant cells[3].

体内研究
(In Vivo)

Retaspimycin (IPI-504, 50 mg/kg, i.v.) causes selective tumor retention in RPMI-8226 tumor-bearing mice[1]. Retaspimycin (IPI-504, 100 mg/kg, p.o., 3 times per week) reduces the tumor volume by 69% and and 84% of baseline values in GIST-882 and GIST-PSW xenografts, respectively. Furthermore, Retaspimycin in combination with imatinib inhibits tumor growth more significantly than Retaspimycin alone in GIST-PSW model, but no obvious difference is ovsrebed in the GIST-882 model. Retaspimycin also downregulates KIT in gastrointestinal stromal tumor (GIST)[2]. Retaspimycin (IPI-504, 50 mg/kg) shows antitumor activity in HCC1569 xenografts. IPI-504 (100 mg/kg, i.p.) effectively decreases the levels of HER2, p-Akt, and p-MAPKs in BT474R and BT474H1047R tumors[3].

Clinical Trial
分子量

587.70

Formula

C31H45N3O8

CAS 号

857402-23-4

中文名称

瑞他霉素

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.