2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. AU-15330

AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity.

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

AU-15330 Chemical Structure

AU-15330 Chemical Structure

CAS No. : 2380274-50-8

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5 mg USD 420 In-stock
10 mg USD 650 In-stock
25 mg USD 1040 In-stock
50 mg USD 1420 In-stock
100 mg USD 1910 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of AU-15330:

AU-15330 Related Antibodies

Top Publications Citing Use of Products

    AU-15330 purchased from MedChemExpress. Usage Cited in: Cell. 2023 Nov 22;186(24):5290-5307.e26.  [Abstract]

    AU-15330 (1 μM; 1, 2, 4, 8 h) rapidly depletes BRG1 and its protein levels become undetectable after 1 hour in MV411 cells.

    View All PROTACs Isoform Specific Products:

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    von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity[1].

    IC50 & Target

    SMARCA2 and SMARCA4[1]
    In Vivo

    AU-15330 (10 and 30 mg/kg; i.v.; 5 days per week for 3 weeks) shows no evident toxicity in immuno-competent mice[1].
    AU-15330 (60 mg/kg with or without 10 mg/kg enzalutamide; i.v.; 3 days per week; p.o.; 5 days per week for 5 weeks) leads to potent inhibition of tumour growth, triggering disease regression in more than 20% of animals. Combinatorial regimen induced the most potent anti-tumour effect, with regression in all animals[1].
    AU-15330 (60 mg/kg with or without 10 mg/kg enzalutamide; i.v.; 3 days per week; p.o.; 5 days per week for 5 weeks) strongly inhibits the growth of C4-2B cell line-derived CRPC xenografts in intact mice as a single agent and synergized with enzalutamide[1].
    AU-15330 (60 mg/kg with or without 10 mg/kg enzalutamide; i.v.; 3 days per week; p.o.; 5 days per week for 5 weeks) combines with enzalutamide induces significant tumour growth inhibition, causing regression in more than 30% of animals in the modle of CRPC variant of the MDA-PCa-146-12 PDX by tumour implantation into castrated mice[1].

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

    Animal Model: Six-week-old male CB17 severe combined immunodeficiency (SCID) mice[1]
    Dosage: 10 and 30 mg/kg
    Administration: i.v. (5 days per week for 3 weeks)
    Result: Showed no evident toxicity in immuno-competent mice.
    Animal Model: VCaP castration-resistant tumour model (six-week-old male CB17 severe combined immunodeficiency (SCID) mice)[1]
    Dosage: 60 mg/kg with or without 10 mg/kg enzalutamide
    Administration: i.v. (3 days per week); p.o. (5 days per week for 5 weeks)
    Result: Resulted inhibition of tumor growth and triggered disease regression in more than 20% of animals. Combinatorial regimen induced the most potent anti-tumour effect, with regression in all animals.
    Animal Model: C4-2B non-castrated tumour model (six-week-old male CB17 severe combined immunodeficiency (SCID) mice)[1]
    Dosage: 60 mg/kg with or without 30 mg/kg enzalutamide
    Administration: i.v. (3 days per week); p.o. (5 days per week for 4 weeks)
    Result: Strongly inhibited the growth of C4-2B cell line-derived CRPC xenografts in intact mice as a single agent and synergized with enzalutamide.
    Molecular Weight

    755.93

    Formula

    C39H49N9O5S
    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    O=C(N(C[C@@H]1O)[C@@H](C1)C(N[C@H](C2=CC=C(C(SC=N3)=C3C)C=C2)C)=O)[C@H](C(C)(C)C)NC(CN4CCN(C(C=C(C(C=CC=C5)=C5O)N=N6)=C6N)CC4)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, stored under nitrogen, away from moisture

    *In solvent : -80°C, 2 years; -20°C, 1 year (stored under nitrogen, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 140 mg/mL (185.20 mM; Need ultrasonic; 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 1.3229 mL 6.6144 mL 13.2287 mL
    5 mM 0.2646 mL 1.3229 mL 2.6457 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 (stored under nitrogen, away from moisture). 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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: ≥ 3.5 mg/mL (4.63 mM); Clear solution

      This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 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: ≥ 3.5 mg/mL (4.63 mM); Clear solution

      This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 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.
    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).

    *In solvent : -80°C, 2 years; -20°C, 1 year (stored under nitrogen, away from moisture)

    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
    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 (stored under nitrogen, away from moisture). 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 1.3229 mL 6.6144 mL 13.2287 mL 33.0718 mL
    5 mM 0.2646 mL 1.3229 mL 2.6457 mL 6.6144 mL
    10 mM 0.1323 mL 0.6614 mL 1.3229 mL 3.3072 mL
    15 mM 0.0882 mL 0.4410 mL 0.8819 mL 2.2048 mL
    20 mM 0.0661 mL 0.3307 mL 0.6614 mL 1.6536 mL
    25 mM 0.0529 mL 0.2646 mL 0.5291 mL 1.3229 mL
    30 mM 0.0441 mL 0.2205 mL 0.4410 mL 1.1024 mL
    40 mM 0.0331 mL 0.1654 mL 0.3307 mL 0.8268 mL
    50 mM 0.0265 mL 0.1323 mL 0.2646 mL 0.6614 mL
    60 mM 0.0220 mL 0.1102 mL 0.2205 mL 0.5512 mL
    80 mM 0.0165 mL 0.0827 mL 0.1654 mL 0.4134 mL
    100 mM 0.0132 mL 0.0661 mL 0.1323 mL 0.3307 mL
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    AU-15330 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:

    AU-153302380274-50-8AU15330AU 15330PROTACsEpigenetic Reader Domaincastration-resistantantitumorPROTACSMARCA2SMARCA4CRPCcastration-resistant prostate cancertoxicityInhibitorinhibitorinhibit

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