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

AT13387 (Synonyms: Onalespib)

Cat. No.: HY-14463 Purity: 99.64%
Data Sheet SDS Handling Instructions

AT13387 is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity.

For research use only. We do not sell to patients.
AT13387 Chemical Structure

AT13387 Chemical Structure

CAS No. : 912999-49-6

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 119 In-stock
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10 mg USD 180 In-stock
50 mg USD 420 In-stock
100 mg USD 684 In-stock
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    AT13387 purchased from MCE. Usage Cited in: Sci Rep. 2017 Mar 15;7(1):201.

    For the caspase 3/7 assay, the HSP90 inhibitor-treated 5637 or SV-HUC cells are stained with Nexcelom ViaStain Caspase 3/7 reagent and Hoechst 33342. Caspase 3/7 positive cells are identified using the Celigo imaging cytometer, and the percentage of apoptotic caspase 3/7 positive cells is calculated with the Celigo software.
    • Biological Activity

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    Description

    AT13387 is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity. IC50 Value: 18 nM Target: Hsp90 in vitro: AT13387 is a synthetic, orally bioavailable, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor AT13387 selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability and degradation of many oncogenic signaling proteins. AT13387 is a selective potent heat shock protein 90 (Hsp90) inhibitor with IC50 of 18 nM in A375 cells. The Kd for AT13387 binding is 0.7 nM. in vivo: AT13387 could be tolerated at doses of up to 70 mg/kg twice weekly or 90 mg/kg once weekly. Body weight loss in mice does not exceed 20% before recovering in all cases except one, and loss is highest following the second dose. Tumor growth inhibition is similar in NCI-H1975 for both dosing regimens. The maintenance of antitumor effects with such a prolonged off-treatment period is consistent with the extended pharmacodynamic action of AT13387 observed for mutant EGFR and other biomarkers in vitro and in vivo and the extended retention of AT13387 in tumors.

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    References
    Molecular Weight

    409.52

    Formula

    C₂₄H₃₁N₃O₃

    CAS No.

    912999-49-6

    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

    Solvent & Solubility

    DMSO: ≥ 33 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Product Name:
    AT13387
    Cat. No.:
    HY-14463
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