Retaspimycin
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.
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- CAS 番号: 857402-23-4
- 分子式: C31H45N3O8
- 分子量:587.70
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
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MedChemExpress（MCE）の使用を引用している文献 Retaspimycin
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生物活性
製品説明
IC50 & Target
[1]|
HSP90 119 nM (EC50) |
GRP94 119 nM (EC50) |
体外実験
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.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
化学情報
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CAS 番号 857402-23-4
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分子量 587.70
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分子式 C31H45N3O8
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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
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (5)
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Journal Impact Factor
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Most Recent
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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.
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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
純度とドキュメンテーション
参考文献
[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]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Retaspimycin 関連分類
HY-15263 関連分類
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