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  3. Tanespimycin

Tanespimycin (Synonyms: 17-AAG; NSC 330507; CP 127374)

Cat. No.: HY-10211 Purity: 99.03%
Handling Instructions

Tanespimycin (17-AAG) est un inhibiteur puissant de HSP90 avec un IC50 de 5 nM, ayant une affinité de liaison 100 fois plus élevée pour la tumeur HSP90 dérivé de cellule que HSP90 dérivé de cellule normale. Tanespimycin épuise les cellules STK38/NDR1 cellulaires et réduit l'activité des kinases STK38. Tanespimycin régule également à la baisse l'expression stk38 du gène.

Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression.

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

Tanespimycin Chemical Structure

Tanespimycin Chemical Structure

CAS No. : 75747-14-7

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10 mM * 1  mL in DMSO USD 79 In-stock
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Customer Review

Based on 14 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Tanespimycin purchased from MCE. Usage Cited in: Mol Cancer Ther. 2016 Sep;15(9):2107-18.

    Combination of MDV3100 and 17-AAG leads to decreased AR protein level and transcriptional activity. (A&B) LNCaP (A) and C4-2 (B) cells are treated as indicated for 24 hr, followed by IB against AR, PSA and CHIP. (C&D) 22RV1 (C) and MR49F (D) cells are treated as indicated for 24 hr, followed by IB against AR and HSP90. (E) C4-2 cells are treated as indicated for 24 hr, fractionated into cytoplasm and nuclear, followed by IB against AR and Plk1.

    Tanespimycin purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Feb 7;9(2):165.

    Western blot analysis of Hsp70 protein and Hsp90 client proteins IKK and EGFR after 24 h Tan IIA treatment. The Hsp90 inhibitor 17-AAG (10 μM) is included as a positive control

    Tanespimycin purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Mar 27;37(1):70.

    Cells are first treated with commercially available HIF-1α inhibitors, including compounds targeting Top1 (Camptothecin, CPT), Top2 (VP; MX) and HSP90 (17-AAG) as well as 2-ME, and then subjected to Western blotting analysis.

    Tanespimycin purchased from MCE. Usage Cited in: Front Mol Neurosci. 2018 Nov 6;11:401.

    Effects of 17-AAG on neurogenesis 4 weeks after SAH.

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    Description

    Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90[1][5]. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression[3].

    IC50 & Target

    HSP90

    5 nM (IC50)

    Autophagy

     

    Mitophagy

     

    In Vitro

    Tanespimycin causes the degradation of HER2, Akt, and both mutant and wild-type AR and the retinoblastoma-dependent G1 growth arrest of prostate cancer cells. Tanespimycin inhibits prostate cancer cell lines with IC50s ranged from 25-45 nM (LNCaP, 25 nM; LAPC-4, 40 nM; DU-145, 45 nM; and PC-3, 25 nM)[1].
    Tanespimycin (0.1-1 μM) induces a nearly complete loss of ErbB2 on ErbB2-overexpressing breast cancer cells[2]. Tanespimycin inhibits cell growth and induces G2/M cell cycle arrest and apoptosis in CCA cells together with the down-regulation of Bcl-2, Survivin and Cyclin B1, and the up-regulation of cleaved PARP[3].

    In Vivo

    Tanespimycin (25-200 mg/kg, i.p.) causes a dose-dependent decline in AR, HER2, and Akt expression in prostate cancer xenografts. Tanespimycin treatment at doses sufficient to induce AR, HER2, and Akt degradation results in the dose-dependent inhibition of androgen-dependent and -independent prostate cancer xenograft growth without toxicity[1].
    Tanespimycin (60 mg/kg) with Rapamycin (30 mg/kg) inhibits A549 and MDA-MB-231 tumor growth and effects tumor cures in MDA-MB-231 tumor-bearing animals by tail vein injection[4].

    Clinical Trial
    Molecular Weight

    585.69

    Formula

    C₃₁H₄₃N₃O₈

    CAS No.

    75747-14-7

    SMILES

    O=C(C(NC(/C(C)=C/C=C\[[email protected]](OC)[[email protected]](/C(C)=C/[[email protected]@H]([[email protected]]([[email protected]](C[[email protected]@H](C1)C)OC)O)C)OC(N)=O)=O)=CC2=O)C1=C2NCC=C

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

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

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 55 mg/mL (93.91 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7074 mL 8.5369 mL 17.0739 mL
    5 mM 0.3415 mL 1.7074 mL 3.4148 mL
    10 mM 0.1707 mL 0.8537 mL 1.7074 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Cell Assay
    [1]

    For the Alamar Blue proliferation assay, 2-4×103 cells are plated in 96-well plates. Later (48 h), cells are treated with Tanespimycin for 96 h or 0.01% DMSO as control. On day 4, Alamar Blue viability assay is performed as described elsewhere. IC50 and IC90s are calculated as the doses of Tanespimycin required to inhibit cell growth by 50 and 90%, respectively. Cell cycle distribution is assayed as described previously with a Becton Dickinson fluorescence-activated cell sorter and analyzed by the Cell Cycle Multicycle system.

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

    Animal Administration
    [1]

    Tanespimycin is dissolved in an EPL vehicle. To aid in the identification of an optimal dose and schedule, nontumor bearing mice are treated by i.p. injection with 25-200 mg/kg of Tanespimycin 5 days/week for 3 weeks or by the EPL vehicle alone. Serum samples are taken from each group, and equal volumes are pooled on days 5, 10, and 15 of treatment for serum chemistry and liver function analysis. At sacrifice, plasma samples are collected for complete blood count. A gross necropsy is performed on all of the mice, and a complete necropsy, including histopathology, is performed on 1 animal/group.

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

    References

    Purity: 99.03%

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    Keywords:

    Tanespimycin17-AAGNSC 330507CP 127374NSC330507NSC-330507CP127374CP-127374HSPAutophagyMitophagyBacterialApoptosisAntibioticHeat shock proteinsMitochondrial AutophagyARHER2A549MDA-MB-231tumorprostatecancerstk38Inhibitorinhibitorinhibit

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    Product Name:
    Tanespimycin
    Cat. No.:
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