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Cat. No.: HY-15263

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Retaspimycin

Name: Retaspimycin
Brand: MedChemExpress
SKU: HY-15263
Availability: PreOrder

5 Cited Publications

Customer Review

Based on 5 publication(s) in Google Scholar

Retaspimycin is a potent inhibitor of Hsp90, with EC₅₀s of 119 nM for both Hsp90 and Grp9.

For research use only. We do not sell to patients.

CAS No.: 857402-23-4
Formula: C₃₁H₄₅N₃O₈
Molecular Weight:587.70

Storage:

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

Data Sheet (278 KB)

Retaspimycin Chemical Structure

CAS No.: 857402-23-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (5)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Retaspimycin is a potent inhibitor of Hsp90, with EC₅₀s of 119 nM for both Hsp90 and Grp9.

IC₅₀ & Target

^[1]

HSP90

119 nM (EC₅₀)

GRP94

119 nM (EC₅₀)

All HSP Isoforms :

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991			2011-05	PHASE1

Chemical Information

CAS No. 857402-23-4
Molecular Weight 587.70
Formula C₃₁H₄₅N₃O₈
SMILES

OC1=C(C[C@H](C[C@@H]([C@@H]2O)OC)C)C(NCC=C)=C(C=C1NC(/C(C)=C/C=C/[C@@H]([C@H](/C(C)=C/[C@@H]2C)OC(N)=O)OC)=O)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Publications (5)

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Signal Transduct Target Ther

Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]

2025 Dec 15;10(1):406. PMID: 41392286
Theranostics

Inhibition of HSP90β Improves Lipid Disorders by Promoting Mature SREBPs Degradation via the Ubiquitin-proteasome System. [Abstract]

2019 Aug 12;9(20):5769-5783. PMID: 31534518
Transl Oncol

Homoharringtonine Combined with the Heat Shock Protein 90 Inhibitor IPI504 in the Treatment of FLT3-ITD Acute Myeloid Leukemia. [Abstract]

2019 Jun;12(6):801-809. PMID: 30953928

Retaspimycin purchased from MedChemExpress. Usage Cited in: Transl Oncol. 2019 Jun;12(6):801-809. [Abstract]

After treated with HHT (8 nM) and/or IPI504 (0.8 μM) for 24 h, MV4-11, MOLM-13 and primary cell lysates are subjected to western blot analysis using the PARP, caspase3 and cleaved caspase3 antibodies, β-actin is displayed as a loading control.
FASEB J

The downregulation of HSP90-controlled CRALBP expression is associated with age-related vision attenuation. [Abstract]

2023 Mar;37(3):e22832. PMID: 36826429
J Cell Biochem

Deficiency of HSF4 Increases the Secretion of Small Extracellular Vesicles via Upregulation of Chaperone-Mediated Autophagy. [Abstract]

2025 Apr;126(4):e70031. PMID: 40211689

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (5)
Purity & Documentation
References

1/16
1/16

Retaspimycin purchased from MedChemExpress. Usage Cited in: Transl Oncol. 2019 Jun;12(6):801-809. [Abstract]

Customer Validation
After treated with HHT (8 nM) and/or IPI504 (0.8 μM) for 24 h, MV4-11, MOLM-13 and primary cell lysates are subjected to western blot analysis using the PARP, caspase3 and cleaved caspase3 antibodies, β-actin is displayed as a loading control.

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Retaspimycin

Publications Citing Use of MedChemExpress (MCE) Retaspimycin

All HSP Isoforms