1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
    Autophagy
  2. HSP
    Autophagy
    Mitophagy

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

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

17-AAG is a potent HSP90 inhibitor with IC50 of 5 nM, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells.

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

17-AAG Chemical Structure

17-AAG Chemical Structure

CAS No. : 75747-14-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
10 mg USD 72 In-stock
Estimated Time of Arrival: December 31
25 mg USD 120 In-stock
Estimated Time of Arrival: December 31
100 mg USD 300 In-stock
Estimated Time of Arrival: December 31
200 mg USD 420 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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Other Forms of 17-AAG:

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

    Combination of Enzalutamide and 17-AAG lead 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.

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

    Western blot analysis of MCF-7 cells treated with Tan IIA at the specified concentrations for the expression of cytosolic PKC isoforms. The compound Go 6983 (GO, 20 μM) is included as a positive control.

    17-AAG 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

    17-AAG 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 (Etoposide, VP; Mitoxantrone, MX) and HSP90 (17-AAG) as well as 2-ME, and then subjected to Western blotting analysis.

    View All HSP Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    17-AAG is a potent HSP90 inhibitor with IC50 of 5 nM, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells.

    IC50 & Target[5]

    HSP90

    5 nM (IC50)

    Autophagy

     

    Mitophagy

     

    In Vitro

    17-AAG causes the degradation of HER2, Akt, and both mutant and wild-type AR and the retinoblastoma-dependent G1 growth arrest of prostate cancer cells. 17-AAG 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]. Combination of 17-AAG (10 nM) and Trastuzumab induces more effective ErbB2-degradation. 17-AAG (0.1-1 μM) induces a nearly complete loss of ErbB2 on ErbB2-overexpressing breast cancer cells[2]. 17-AAG 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

    17-AAG (25-200 mg/kg, i.p.) causes a dose-dependent decline in AR, HER2, and Akt expression in prostate cancer xenografts. 17-AAG 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]. 17-AAG (60 mg/kg) with paclitaxel (60 mg/kg) and rapamycin (30 mg/kg) inhibits A549 and MDA-MB-231 tumor growth far more potently than paclitaxel-containing micelles and effected tumor cures in MDA-MB-231 tumor-bearing animals by tail vein injection[4].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 55 mg/mL (93.91 mM)

    *"≥" 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 17-AAG 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 17-AAG 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]

    17-AAG 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 17-AAG 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
    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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.03%

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    Product Name:
    17-AAG
    Cat. No.:
    HY-10211
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    17-AAG

    Cat. No.: HY-10211