1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  2. HSP
  3. Retaspimycin

Retaspimycin 

Cat. No.: HY-15263
Handling Instructions

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.

Retaspimycin Chemical Structure

Retaspimycin Chemical Structure

CAS No. : 857402-23-4

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of Retaspimycin:

Other Forms of Retaspimycin:

Top Publications Citing Use of Products

    Retaspimycin 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.

    View All HSP Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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)

    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
    Molecular Weight

    587.70

    Formula

    C31H45N3O8

    CAS No.
    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.

    Purity & Documentation
    References
    Cell Assay
    [3]

    Cell proliferation is studied using the cell proliferation reagent WST-1. Briefly, 8 × 103 cells are seeded in triplicate in 96-well plates and treated for 5 days, with either trastuzumab or Retaspimycin as indicated. Viable cells are estimated on the basis of their ability to metabolize tetrazolium salt WST-1 to formazan by mitochondrial dehydrogenases. Quantification of the formazan dye directly correlates with the number of metabolically active cells and is analyzed by a scanning microplate reader. Results are shown as means ± SE[3].

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

    Animal Administration
    [1]

    RPMI-8226 cells are harvested from cultures grown in vitro in RPMI medium 1640 supplemented with heat-inactivated 10% (wt/vol) FBS and 100 units/mL penicillin/streptomycin at 37°C under a humidified 95%/5% (vol/vol) mixture of air and CO2. Cells are washed twice by using sterile Hepes-buffered saline (HBS) and suspended in HBS to a concentration of 1 × 108 viable cells per mL. Twelve female Nu/Nu nude mice (≈20 g) are used in the assay. RPMI-8226 cells (1 × 107 cells per mouse) are implanted in the right flank. When tumor volume reaches ≈200-500 mm3 (≈4 weeks postimplantation), animals receive a single i.v. dose of 50 mg/kg Retaspimycin via the tail vein. At 4, 24, and 48 h posttreatment, the animals are killed with carbon dioxide, and tumors are removed and stored at −80°C until analyzed. Four animals are used for each time point. Tumor samples are homogenized in an ice-cold, nitrogen-sparged 1:1 solution of MeOH:150 mM citrate, 0.2% (wt/vol) EDTA, and 0.2% (wt/vol) ascorbate (pH 3.0) for 1 min in an ice/water bath with a homogenizer at 17,500 rpm. Samples are centrifuged for 5 min at 4°C at 18,000 × g. The supernatants are diluted 1:1 with ice-cold, nitrogen-sparged 75 mM citrate, 0.1% (wt/vol) EDTA, and 0.1% (wt/vol) ascorbate (pH 3) containing 25 ng/mL deuterated 17-AAG as internal standard and analyzed by LC-MS/MS analysis. The standard curve is prepared for Retaspimycin, 17-AAG, and 17-AG in 1:1 MeOH:150 mM citrate, 0.2% (wt/vol) EDTA, and 0.2% (wt/vol) ascorbate (pH 3.0); diluted 1:1 with ice-cold, nitrogen-sparged 75 mM citrate, 0.1% (wt/vol) EDTA, and 0.1% (wt/vol) ascorbate (pH 3.0) containing 25 ng/mL deuterated 17-AAG as internal standard; and analyzed by LC-MS/MS[1].

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

    References
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Retaspimycin Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Salutation

    Applicant Name *

     

    Email Address *

    Phone Number *

     

    Organization Name *

    Department *

     

    Requested quantity *

    Country or Region *

         

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Retaspimycin
    Cat. No.:
    HY-15263
    Quantity:
    MCE Japan Authorized Agent: