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

AT13387 (Synonyms: Onalespib)

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

AT13387 is a potent inhibitor of Hsp90, with Kd of 0.71 nM.

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

AT13387 Chemical Structure

AT13387 Chemical Structure

CAS No. : 912999-49-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 119 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
50 mg USD 420 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
100 mg USD 684 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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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.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    AT13387 is a potent inhibitor of Hsp90, with Kd of 0.71 nM.

    IC50 & Target[1]

    HSP90

    0.71 nM (Kd)

    In Vitro

    AT13387 (Compound 35) is a potent inhibitor of Hsp90, with Kd of 0.71 nM. AT13387 shows potent antiproliferative activity in HCT116 cells, with an IC50 of 31 nM. AT13387 also strongly inhibits the proliferation of a panel of human tumor cell lines, showing IC50 of < 100 nM[1]. AT13387 exhibits cytotoxic activity against many of the PPTP cell lines, with median IC50 of 41 nM[2].

    In Vivo

    AT13387 (60 mg/kg, ip 3 days on and 3 days off for four cycles) shows antitumor activity in nude BALB/c mice bearing early stage HCT116 human colon carcinoma xenografts[1]. AT13387 (40 or 60 mg/kg, i.p.) induces significant differences in EFS distribution compared to controls in 17% evaluable solid tumor xenografts, but in none of the ALL xenografts[2].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 33 mg/mL (80.58 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4419 mL 12.2094 mL 24.4188 mL
    5 mM 0.4884 mL 2.4419 mL 4.8838 mL
    10 mM 0.2442 mL 1.2209 mL 2.4419 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Cell Assay
    [2]

    In vitro testing is performed using DIMSCAN. Cells are incubated in the presence of AT13387 for 96 hours at concentrations from 1 nM to 10 μM[2].

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

    Animal Administration
    [1]

    HCT116 cells are injected SC into the right hind flank of male nude BALB/c mice. Tumours are apparent 7 to 10 days later. Mice are arranged into matched groups of 12 according to tumour volume giving a group mean of approximately 100 mm[3] at initiation of dosing. Tumour volumes are measured every 2 days. Statistical significance between groups is assessed using nonparametric one-way ANOVA. Mice are given the lactate salt of AT13387 using a repeated cycle of dosing of once per day for three days, no dose for three days, once per day for three days etc., for four dosing cycles at 60 mg/kg/dose (as free base equivalents) dissolved in 17.5% hydroxypropyl-β-cyclodextrin via the IP route. Control mice receive dose vehicle only via the same route. Tolerability is assessed by recording body weight, clinical observations and survival[1].

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

    References
    Molecular Weight

    409.52

    Formula

    C₂₄H₃₁N₃O₃

    CAS No.

    912999-49-6

    SMILES

    OC1=CC(O)=C(C(C)C)C=C1C(N2CC(C=CC(CN3CCN(C)CC3)=C4)=C4C2)=O

    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

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

    Cat. No.: HY-14463