2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP
  4. Onalespib

Onalespib (AT13387) is a long-acting second-generation Hsp90 inhibitor with a Kd of 0.71 nM.

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

Onalespib Chemical Structure

Onalespib Chemical Structure

CAS No. : 912999-49-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 131 In-stock
Solution
10 mM * 1 mL in DMSO USD 131 In-stock
Solid
1 mg USD 48 In-stock
5 mg USD 119 In-stock
10 mg USD 198 In-stock
50 mg USD 462 In-stock
100 mg USD 752 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Onalespib:

Onalespib Related Antibodies

Top Publications Citing Use of Products

    Onalespib purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Mar 15;7(1):201.  [Abstract]

    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.

    View All HSP Isoform Specific Products:

    View All Isoforms
    HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Onalespib (AT13387) is a long-acting second-generation Hsp90 inhibitor with a Kd of 0.71 nM.

    IC50 & Target[1]

    HSP90

    0.71 nM (Kd)

    In Vitro

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

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

    Onalespib Related Antibodies
    In Vivo

    Onalespib (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]. Onalespib (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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    409.52

    Formula

    C24H31N3O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (122.09 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.10 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.10 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 16.67 mg/mL (40.71 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.62%

    COA (247 KB) LCMS (260 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    In vitro testing is performed using DIMSCAN. Cells are incubated in the presence of Onalespib 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 Onalespib 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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4419 mL 12.2094 mL 24.4188 mL 61.0471 mL
    5 mM 0.4884 mL 2.4419 mL 4.8838 mL 12.2094 mL
    10 mM 0.2442 mL 1.2209 mL 2.4419 mL 6.1047 mL
    15 mM 0.1628 mL 0.8140 mL 1.6279 mL 4.0698 mL
    20 mM 0.1221 mL 0.6105 mL 1.2209 mL 3.0524 mL
    25 mM 0.0977 mL 0.4884 mL 0.9768 mL 2.4419 mL
    30 mM 0.0814 mL 0.4070 mL 0.8140 mL 2.0349 mL
    40 mM 0.0610 mL 0.3052 mL 0.6105 mL 1.5262 mL
    50 mM 0.0488 mL 0.2442 mL 0.4884 mL 1.2209 mL
    60 mM 0.0407 mL 0.2035 mL 0.4070 mL 1.0175 mL
    80 mM 0.0305 mL 0.1526 mL 0.3052 mL 0.7631 mL
    100 mM 0.0244 mL 0.1221 mL 0.2442 mL 0.6105 mL
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    Onalespib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Onalespib912999-49-6AT13387AT 13387AT-13387HSPHeat shock proteinsInhibitorinhibitorinhibit

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