包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Cell lines | Glioma cell lines (D-54 MG and U-251 MG cells) |
Preparation method | This compound was soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reaction Conditions | 1 or 2.5 μM; 24 or 48 hrs |
Applications | In glioma cells, IPI-504 inhibited cell proliferation through increasing sub-G1 population of cells and dose-dependently inducing fragmented DNA of the apoptotic cells. |
Animal models | Mice bearing human brain tumor D-54MG xenografts |
Dosage form | 100 mg/kg; i.p.; b.i.d., twice weekly or 5/2/5 schedule (5 days on, 2 days off, and then 5 days on), for 6 weeks |
Applications | In immunocompromised mice, IPI-504 mildly attenuated tumor growth. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
产品描述 | Retaspimycin hydrochloride (also known as IPI-504), a hydroquinone hydrochloride salt derivative of 17-AAG, is a novel, potent and selective inhibitor of heat shock protein 90(Hsp90) that binds to the amino-terminal ATP/ADP-binding site of Hsp90. As a highly water-soluble version of 17-AAG, IPI-504 (solubility > 200 mg/mL) does not need prior dissolution in organic solvents and hence can be delivered in high concentrations. Once in the systemic circulation, IPI-504 is deprotonated and converted into the free base IPI-504 which is subsequently oxidized to 17-AAG. IPI-504 potently inhibits proliferation in several tumor cell lines with 50% inhibition concentration IC50values ranging from 10-40 nmol/L and has been used for the treatment of gastrointestinal stromal tumors, soft-tissue sarcomas and non-small cell lung cancer. Reference [1].Britt Erika Hanson and David H Vesole. Retaspimycin hydrochloride (IPI-504): a novel heat shock protein inhibitor as an anticancer agent. Expert Opin. Investi. Drugs (2009) 18(9): 1375-1383 |