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

Onalespib  (Synonyms: AT13387)

Cat. No.: HY-14463 Purity: 99.62%
COA Handling Instructions

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

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 131 In-stock
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10 mM * 1 mL in DMSO USD 131 In-stock
Solid
5 mg USD 119 In-stock
10 mg USD 198 In-stock
50 mg USD 462 In-stock
100 mg USD 752 In-stock
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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

    Appearance

    Solid

    Formula

    C24H31N3O3
    CAS No.
    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)

    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.
    In Vivo:
    • 1.

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

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

    • 2.

      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

    • 3.

      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

    • 4.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    *All of the co-solvents are available by MedChemExpress (MCE).
    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
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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.

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    Keywords:

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

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