Art. -Nr.: HY-145388

AU-15330

15 Cited Publications

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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).

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Reinheit: 99.89%
CAS. Nr.: 2380274-50-8
Formel: C₃₉H₄₉N₉O₅S
Molecular Weight:755.93

Speicherung:

4°C, stored under nitrogen, away from moisture

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

AU-15330 Chemical Structure

CAS. Nr.: 2380274-50-8

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vivo
Chemical Information
Publications (15)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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]. (Pink: Target protein ligand; Blue: VHL ligand (HY-112078); Black: linker).

IC₅₀ & Target^[1]

VHL

SMARCA2

SMARCA4

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle SWI/SNF Complex Isoform-spezifische Produkte anzeigen :

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.

Chemical Information

CAS. Nr. 2380274-50-8
Appearance Solid
Molecular Weight 755.93
Formel C₃₉H₄₉N₉O₅S
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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)

All WBBio/Physico-chemical AssayCell Proliferation/Viability Assay

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Journal Impact Factor

Cancer Cell

IRF4 requires ARID1A to establish plasma cell identity in multiple myeloma. [Abstract]

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.
Cell

p53 safeguards chemical reprogramming of human somatic cells toward pluripotency. [Abstract]

2026 Jun 11;189(12):3541-3552.e18. PMID: 41999746
Cell

Global identification of SWI/SNF targets reveals compensation by EP400. [Abstract]

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.
Nat Cell Biol

Cis and trans regulatory mechanisms of extrachromosomal DNA segregation. [Abstract]

2026 Jun 24. PMID: 42342951
Mol Cell

β-catenin functions as a molecular adapter for disordered cBAF interactions. [Abstract]

2025 Aug 21;85(16):3041-3056.e9. PMID: 40695292
Nat Commun

Long non-coding RNAs direct the SWI/SNF complex to cell type-specific enhancers. [Abstract]

2025 Jan 2;16(1):131. PMID: 39747144
Sci Adv

BRD9 functions as a methylarginine reader to regulate AKT-EZH2 signaling. [Abstract]

2025 Apr 25;11(17):eads6385. PMID: 40279411
Sci Adv

SMARCA4 regulates the NK-mediated killing of senescent cells. [Abstract]

2025 Jan 17;11(3):eadn2811. PMID: 39813356
Mol Ther

LINC00607 facilitates endothelial VEGF-A receptor FLT1 splicing. [Abstract]

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
bioRxiv

2025 April 16.
bioRxiv

2025 January 02.
bioRxiv

2024 Mar 22.
bioRxiv

2023 Mar 7.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.3229 mL

6.6144 mL

13.2287 mL

5 mM

0.2646 mL

1.3229 mL

2.6457 mL

10 mM

0.1323 mL

0.6614 mL

1.3229 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

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

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

This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Xiao L, et al. Targeting SWI/SNF ATPases in enhancer-addicted prostate cancer. Nature. 2022;601(7893):434-439. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

AU-15330

15 Cited Publications

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AU-15330

PROTAC Library

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) AU-15330

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle SWI/SNF Complex Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (15)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AU-15330

PROTAC Library

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) AU-15330

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle SWI/SNF Complex Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (15)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AU-15330 Related Classifications

HY-145388 Related Classifications