AU-15330
Based on 15 publication(s) in Google Scholar
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.
(Pink: Target protein ligand; Blue: VHL ligand (HY-112078); Black: linker).
For research use only. We do not sell to patients.
- Purity : 99.89%
- CAS No.: 2380274-50-8
- Formula: C39H49N9O5S
- Molecular Weight:755.93
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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)
Publications Citing Use of MedChemExpress (MCE) AU-15330
More- Cancer Cell. 2024 Jul 8;42(7):1185-1201.e14. [Abstract]
- Cell. 2026 Jun 11;189(12):3541-3552.e18. [Abstract]
- Cell. 2023 Nov 22;186(24):5290-5307.e26. [Abstract]
- Nat Cell Biol. 2026 Jun 24. [Abstract]
- Nat Commun. 2025 Jan 2;16(1):131. [Abstract]
- Mol Cell. 2025 Aug 21;85(16):3041-3056.e9. [Abstract]
- Sci Adv. 2025 Apr 25;11(17):eads6385. [Abstract]
- Sci Adv. 2025 Jan 17;11(3):eadn2811. [Abstract]
- Mol Ther. 2026 Jul 1;34(7):4323-4338. [Abstract]
- JCI Insight. 2025 Nov 24;10(22):e187448. [Abstract]
- bioRxiv. 2026 Apr 13:2026.04.11.717899. [Abstract]
- bioRxiv. 2025 April 16.
- bioRxiv. 2025 January 02.
- bioRxiv. 2024 Mar 22.
- bioRxiv. 2023 Mar 7.
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WB
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Bio/Physico-chemical Assay
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WB
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Bio/Physico-chemical Assay
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Cell Proliferation/Viability Assay
All PROTACs Isoforms
MoreAll SWI/SNF Complex Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
VHL |
SMARCA2 |
SMARCA4 |
In Vivo
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.
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Animal Model:Six-week-old male CB17 severe combined immunodeficiency (SCID) mice[1]
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Dosage:10 and 30 mg/kg
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Administration:i.v. (5 days per week for 3 weeks)
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Result:Showed no evident toxicity in immuno-competent mice.
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Animal Model:VCaP castration-resistant tumour model (six-week-old male CB17 severe combined immunodeficiency (SCID) mice)[1]
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Dosage:60 mg/kg with or without 10 mg/kg enzalutamide
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Administration:i.v. (3 days per week); p.o. (5 days per week for 5 weeks)
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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.
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Animal Model:C4-2B non-castrated tumour model (six-week-old male CB17 severe combined immunodeficiency (SCID) mice)[1]
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Dosage:60 mg/kg with or without 30 mg/kg enzalutamide
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Administration:i.v. (3 days per week); p.o. (5 days per week for 4 weeks)
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Result:Strongly inhibited the growth of C4-2B cell line-derived CRPC xenografts in intact mice as a single agent and synergized with enzalutamide.
Chemical Information
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CAS No. 2380274-50-8
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Appearance Solid
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Molecular Weight 755.93
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Formula C39H49N9O5S
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Color Off-white to yellow
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)
Publications (15)
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Journal Impact Factor
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Most Recent
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Cancer Cell
2024 Jul 8;42(7):1185-1201.e14. PMID: 38906156
AU-15330 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2024 Jul 8;42(7):1185-1201.e14. [Abstract]
Western Blot analysis was performed in NCI-H929 and SKMM1 after AU-15330 (24 h) treatment. AU-15330 caused the loss of both IRF4 and MYC proteins in MM lines.
AU-15330 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2024 Jul 8;42(7):1185-1201.e14. [Abstract]
Heatmap of identified ATAC-seq peaks in SKMM1, NCI-H929, and a MM patient sample treated with DMSO or AU-15330 (1 μM; 2.5 h). AU-15330 treatment led to a global loss of chromatin accessibility in MM cells among enriched ATAC peaks.
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Cell
2026 Jun 11;189(12):3541-3552.e18. PMID: 41999746 -
Cell
2023 Nov 22;186(24):5290-5307.e26. PMID: 37922899
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.
AU-15330 purchased from MedChemExpress. Usage Cited in: Cell. 2023 Nov 22;186(24):5290-5307.e26. [Abstract]
Heatmap representation of the effects of AU-15330 (1 h) treatment on ATAC-seq signal at MV411 enhancers. AU-15330 caused a rapid loss of accessibility of enhancers in MV411 cells.
AU-15330 purchased from MedChemExpress. Usage Cited in: Cell. 2023 Nov 22;186(24):5290-5307.e26. [Abstract]
Drug dose response curves of wildtype and EP400-KO A549 cells following treatment with AU-15330 (8 d) and quantification of IC50 values from the dose response curves.
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Nat Cell Biol
2026 Jun 24. PMID: 42342951 -
Nat Commun
2025 Jan 2;16(1):131. PMID: 39747144 -
Mol Cell
2025 Aug 21;85(16):3041-3056.e9. PMID: 40695292 -
Sci Adv
2025 Apr 25;11(17):eads6385. PMID: 40279411 -
Sci Adv
2025 Jan 17;11(3):eadn2811. PMID: 39813356 -
Mol Ther
2026 Jul 1;34(7):4323-4338. PMID: 41935951 -
JCI Insight
Mitochondrial metabolic rewiring sensitizes mTORC1 inhibitor persister cells to cuproptosis. [Abstract]2025 Nov 24;10(22):e187448. PMID: 41277553 -
bioRxiv
ARID1A deficiency unleashes centromeric RNA transcription to drive chromosomal instability and boosts PKMYT1 inhibitor efficacy via RNA sensing. [Abstract]2026 Apr 13:2026.04.11.717899. PMID: 42039593 -
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Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (132.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.31 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.31 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocols
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Splenic/Portal-Vein Liver Metastasis Xenograft
Splenic and portal-vein liver metastasis xenograft models deliver tumor cells into the portal circulation so that cells reach the liver first and form hepatic metastatic lesions; splenic injection uses the spleen as an access route to the portal system, while direct portal-vein injection introduces cells into the portal vein without requiring splenectomy. The assay detects liver colonization, intrahepatic tumor growth, tumor distribution, treatment response, survival, and liver-metastasis microenvironment changes; readouts include bioluminescence or fluorescence imaging, gross liver nodule counts, liver weight or tumor burden, histology, and survival.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
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Intraperitoneal/Peritoneal Dissemination Xenograft
Intraperitoneal (IP) or peritoneal dissemination xenograft models are based on the introduction of human cancer cells into the peritoneal cavity of immunodeficient mice, where they attach to peritoneal surfaces, form multicellular aggregates or spheroids, and progressively generate disseminated tumor nodules that mimic advanced peritoneal metastatic disease. These models are widely used to study ovarian cancer progression, tumor-microenvironment interactions, and intraperitoneal therapeutic responses, often incorporating bioluminescence or fluorescence imaging to longitudinally monitor tumor burden in vivo. The biological principle relies on the capacity of tumor cells such as SKOV3 or related ovarian carcinoma lines to survive in suspension, aggregate within ascites-like fluid, adhere to mesothelial surfaces, and invade peritoneal organs, thereby recapitulating human peritoneal carcinomatosis patterns observed in advanced disease.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
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 |