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

Retaspimycin 

Cat. No.: HY-15263
Handling Instructions

Retaspimycin is a potent and water-soluble 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

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Top Publications Citing Use of Products

    Retaspimycin purchased from MCE. Usage Cited in: Transl Oncol. 2019 Apr 3;12(6):801-809.

    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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    Description

    Retaspimycin is a potent and water-soluble 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].

    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].

    Clinical Trial
    Molecular Weight

    587.70

    Formula

    C₃₁H₄₅N₃O₈

    CAS No.

    857402-23-4

    SMILES

    OC1=C(C[[email protected]](C[[email protected]@H]([[email protected]@H]2O)OC)C)C(NCC=C)=C(C=C1NC(/C(C)=C/C=C/[[email protected]@H]([[email protected]](/C(C)=C/[[email protected]@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.

    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
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    Keywords:

    RetaspimycinHSPHeat shock proteinsInhibitorinhibitorinhibit

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