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Retaspimycin

Catalog No. T12726 CAS 857402-23-4

Retaspimycin is a potent and water-soluble Hsp90 inhibitor(EC50s of 119 nM for both Hsp90 and Grp9).

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Retaspimycin, CAS 857402-23-4

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Retaspimycin is a potent and water-soluble Hsp90 inhibitor(EC50s of 119 nM for both Hsp90 and Grp9).
Targets&IC50	HSP90:119 nM （EC50）, Grp94:119 nM （EC50）
In vitro	Retaspimycin is a potent Hsp90 inhibitor(EC50s of 119 nM for both Hsp90 and Grp9). Retaspimycin is cytocoxic to human multiple myeloma (MM) cell lines(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].
In vivo	selective tumor retention in RPMI-8226 tumor-bearing mice caused by Retaspimycin. The tumor volume by 69% and and 84% of baseline values in GIST-882 and GIST-PSW xenografts reduced by Retaspimycin, 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]

Molecular Weight	587.7
Formula	C31H45N3O8
CAS No.	857402-23-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Sydor JR, et al. Development of 17-allylamino-17-demethoxygeldanamycin hydroquinone hydrochloride (IPI-504), an anti-cancer agent directed against Hsp90. Proc Natl Acad Sci U S A. 2006 Nov 14;103(46):17408-13. Epub 2006 Nov 7. 2. Floris G, et al. The heat shock protein 90 inhibitor IPI-504 induces KIT degradation, tumor shrinkage, and cell proliferation arrest in xenograft models of gastrointestinal stromal tumors. Mol Cancer Ther. 2011 Oct;10(10):1897-908. 3. Scaltriti M, et al. Antitumor activity of the Hsp90 inhibitor IPI-504 in HER2-positive trastuzumab-resistant breast cancer. Mol Cancer Ther. 2011 May;10(5):817-24.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Retaspimycin 857402-23-4 Others inhibitor inhibit

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