Retaspimycin Hydrochloride
Based on 5 publication(s) in Google Scholar
Retaspimycin Hydrochloride is a potent inhibitor of Hsp90 with EC50s of 119 nM for both Hsp90 and Grp9.
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- Purity: 95.49%
- CAS No.: 857402-63-2
- 화학식: C31H46ClN3O8
- 분자량:624.17
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보관:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Retaspimycin Hydrochloride
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WB
Biological Activity
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HSP90 119 nM (EC50) |
GRP94 119 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H3122 | GI50 |
76 nM
Compound: 4; IPI-504
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Cytotoxicity against crizotinib-resistant human NCI-H3122 cells assessed as cell growth inhibition after 72 hrs by trypan blue exclusion assay
Cytotoxicity against crizotinib-resistant human NCI-H3122 cells assessed as cell growth inhibition after 72 hrs by trypan blue exclusion assay
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[PMID: 26844689] |
| SK-BR-3 | EC50 |
20 nM
Compound: 1a
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Degradation of Her2 in SKBR3 cells
Degradation of Her2 in SKBR3 cells
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[PMID: 16854066] |
| SK-BR-3 | EC50 |
22 nM
Compound: 1a
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Upregulation of Hsp70 in SKBR3 cells
Upregulation of Hsp70 in SKBR3 cells
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[PMID: 16854066] |
| SK-BR-3 | GI50 |
22 nM
Compound: 1a
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Inhibition of human SKBR3 cell growth
Inhibition of human SKBR3 cell growth
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[PMID: 16854066] |
| SK-OV-3 | EC50 |
16 nM
Compound: 1a
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Upregulation of Hsp70 in SKOV3 cells
Upregulation of Hsp70 in SKOV3 cells
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[PMID: 16854066] |
| SK-OV-3 | EC50 |
27 nM
Compound: 1a
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Degradation of Her2 in SKOV3 cells
Degradation of Her2 in SKOV3 cells
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[PMID: 16854066] |
| SK-OV-3 | GI50 |
52 nM
Compound: 1a
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Inhibition of human SKOV3 cell growth
Inhibition of human SKOV3 cell growth
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[PMID: 16854066] |
Retaspimycin (IPI-504) is a novel and highly soluble analog of 17AAG, 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. The IC50s for the inhibition of reporter gene activity by Retaspimycin are 196±56 nM in U266 and 472±177 nM in MM.1s for UPRE-luc activity and 213±140 nM for the ERSE-driven activity in MM.1s cells. Retaspimycin treatment leads to a dose-dependent decrease of p50ATF6 with EC50 of 237 nM, consistent with the reporter-gene assay. The level of sXBP1 is decreased in the presence of Retaspimycin with an apparent EC50 between 300 nM and 1 μM[1]. Incubation of Retaspimycin (IPI-504) 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 857402-63-2
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Appearance Solid
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분자량 624.17
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화학식 C31H46ClN3O8
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Color White to light yellow
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SMILES
O=C(NC1=C2O)/C(C)=C/C=C\[C@H](OC)[C@H](/C(C)=C/[C@@H]([C@H]([C@H](C[C@@H](CC2=C(C(O)=C1)NCC=C)C)OC)O)C)OC(N)=O.Cl
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Synonyms
IPI-504
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 -
FASEB J
The downregulation of HSP90-controlled CRALBP expression is associated with age-related vision attenuation. [Abstract]2023 Mar;37(3):e22832. PMID: 36826429 -
Transl Oncol
Homoharringtonine Combined with the Heat Shock Protein 90 Inhibitor IPI504 in the Treatment of FLT3-ITD Acute Myeloid Leukemia. [Abstract]2019 Apr 3;12(6):801-809. PMID: 30953928
Retaspimycin Hydrochloride purchased from MedChemExpress. Usage Cited in: Transl Oncol. 2019 Apr 3;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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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
용액&용해도
DMSO : 100 mg/mL (160.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.01 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.01 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Hela cells are grown in Dulbecco’s modified Eagle’s medium containing 10% fetal bovine serum, 1 ug/mL streptomycin and 1 ug/mL penicillin. U266 and MM.1s are cultured in RPMI 1640 medium containing 15% fetal bovine serum, 1 mM pyruvate, 1 ug/mL streptomycin, and 1 ug/mL penicillin. All the cell lines are maintained at 37°C in a humidified 5% CO2 atmosphere. Viability studies are performed using the vital mitochondrial function stain Alamar Blue. After cells are incubated in 96-well plates (200 μL) ± Retaspimycin, 20 μL of Alamar Blue is added and incubated for 4-6 h at 37°C. The Alamar Blue reduction is monitored using an Envision plate reader at λEM=544 nm and λEM=590 nm. The ratios obtained from drug-treated cells versus vehicle treated cells are quantified and plotted against drug concentration to give EC50 values. Caspase-3 and 7 activities are detected using the Caspase Glow kit[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
For all the experiments, 2×107 cells are injected into the right flanks of 10 mice for each experimental condition. Established tumors are treated with Trastuzumab, Retaspimycin, or the combination as following: Trastuzumab (10 mg/kg in sterile PBS) or sterile PBS (control) is given intraperitoneally twice weekly. Retaspimyci (100 mg/kg) is administered intraperitoneally thrice weekly. Retaspimyci, Trastuzumab, and the combination treatments are tolerable. No significant toxicity is noticed among the treatment arms. Tumor growth is measured with digital calipers as indicated and tumor volume is determined using the formula: (length×width2)×(π/6). At the end of the experiments, the animals are anesthetized with 1.5% isofluorane-air mixture and killed by cervical dislocation. Results are depicted as means of tumor volume±SE.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (285 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
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- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6021 mL | 8.0106 mL | 16.0213 mL | 40.0532 mL |
| 5 mM | 0.3204 mL | 1.6021 mL | 3.2043 mL | 8.0106 mL | |
| 10 mM | 0.1602 mL | 0.8011 mL | 1.6021 mL | 4.0053 mL | |
| 15 mM | 0.1068 mL | 0.5340 mL | 1.0681 mL | 2.6702 mL | |
| 20 mM | 0.0801 mL | 0.4005 mL | 0.8011 mL | 2.0027 mL | |
| 25 mM | 0.0641 mL | 0.3204 mL | 0.6409 mL | 1.6021 mL | |
| 30 mM | 0.0534 mL | 0.2670 mL | 0.5340 mL | 1.3351 mL | |
| 40 mM | 0.0401 mL | 0.2003 mL | 0.4005 mL | 1.0013 mL | |
| 50 mM | 0.0320 mL | 0.1602 mL | 0.3204 mL | 0.8011 mL | |
| 60 mM | 0.0267 mL | 0.1335 mL | 0.2670 mL | 0.6676 mL | |
| 80 mM | 0.0200 mL | 0.1001 mL | 0.2003 mL | 0.5007 mL | |
| 100 mM | 0.0160 mL | 0.0801 mL | 0.1602 mL | 0.4005 mL |
Retaspimycin Hydrochloride Related Classifications
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