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Retaspimycin Hydrochloride

Catalog No. T12726L CAS 857402-63-2

Synonyms: IPI-504

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

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Retaspimycin Hydrochloride Chemical Structure

Retaspimycin Hydrochloride, CAS 857402-63-2

Pack Size	Availability	Price/USD
2 mg	5 days	$ 107.00
5 mg	5 days	$ 177.00
10 mg	5 days	$ 327.00
50 mg	6-8 weeks	$ 747.00
100 mg	6-8 weeks	$ 1,250.00
1 mL * 10 mM (in DMSO)	5 days	$ 264.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Retaspimycin Hydrochloride is a potent and water-soluble Hsp90 inhibitor(Hsp90 and Grp9 with EC50s of 119 nM).
Targets&IC50	HSP90:119 nM （EC50）, Grp94:119 nM （EC50）
In vitro	Retaspimycin is an inhibitor of Hsp90. Retaspimycin can abrogate both the unfolded protein response element (UPRE) and ERSE-driven luciferase activity in non-treated U266 and MM.1s cells as well as in Tunicamycin (Tm)-treated cells. Incubation of Retaspimycin potently suppresses both Akt and MAPKs phosphorylation in both sensitive and Trastuzumab-resistant cells. Total levels of Akt decreased in all 4 cell lines (BT474, SKBR-3, HCC1569, and HCC1569) in a dose-dependent manner. However, levels of total MAPKs are not significantly altered with Retaspimycin treatment[2].
In vivo	Tumor regression of Trastuzumab-sensitive BT474 cell-derived xenografts independently induceed by Retaspimycin and Trastuzumab. Xenografts derived from BT474R cells continue to grow in the presence of Trastuzumab but are still sensitive to Retaspimycin. When used in combination, Retaspimycin and Trastuzumab add only marginal benefits to Retaspimycin monotherapy. Retaspimycin as a single agent is more efficacious than Trastuzumab in inhibiting tumor growth in HCC1569 xenografts[2].

Synonyms	IPI-504
Molecular Weight	624.17
Formula	C31H46ClN3O8
CAS No.	857402-63-2

Storage

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

Solubility Information

DMSO: 56 mg/mL (89.72 mM)

References and Literature

1. Patterson J, et al. IPI-504, a novel and soluble HSP-90 inhibitor, blocks the unfolded protein response in multiple myeloma cells. Cancer Chemother Pharmacol. 2008 May;61(6):923-32. 2. 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. 3. 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.

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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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Tech Support

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 Hydrochloride 857402-63-2 Others IPI-504 IPI504 IPI 504 inhibitor inhibit

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