Cat. No.: HY-163410

AU-24118

Name: AU-24118
Brand: MedChemExpress
SKU: HY-163410
Price: 600.00 USD
Availability: InStock
Rating: 5 (2 reviews)

2 Cited Publications

고객리뷰

Based on 2 publication(s) in Google Scholar

AU-24118 is an orally active PROTAC degrader that recruits cereblon to target the degradation of SMARCA2, SMARCA4 and PBRM1. AU-24118 impairs the chromatin accessibility of oncogenic transcription factors, inhibits colony formation, dislodges chromatin-bound transcription factors, attenuates downstream signal transduction, induces apoptosis, and exerts antiproliferative and cytotoxic effects. AU-24118 can be used in research related to castration-resistant prostate cancer, colorectal cancer, small cell lung cancer and multiple myeloma (including the t (4;14) subtype).
(Pink: SMARCA2 and SMARCA4 and PNRM1 ligand (HY-171774); Blue: Cereblon ligand (HY-171775); Black: linker).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 98.82%
CAS No.: 3084244-26-5
화학식: C₃₇H₄₀N₆O₄
분자량:632.75

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

AU-24118 Chemical Structure

CAS No.: 3084244-26-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Publications (2)
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

AU-24118 is an orally active PROTAC degrader that recruits cereblon to target the degradation of SMARCA2, SMARCA4 and PBRM1. AU-24118 impairs the chromatin accessibility of oncogenic transcription factors, inhibits colony formation, dislodges chromatin-bound transcription factors, attenuates downstream signal transduction, induces apoptosis, and exerts antiproliferative and cytotoxic effects. AU-24118 can be used in research related to castration-resistant prostate cancer, colorectal cancer, small cell lung cancer and multiple myeloma (including the t (4;14) subtype)^[1]^[2]^[3]^[4]. (Pink: SMARCA2 and SMARCA4 and PNRM1 ligand (HY-171774); Blue: Cereblon ligand (HY-171775); Black: linker).

IC₅₀ & Target

^[1]

SMARCA2

SMARCA4

PBRM1

All PROTACs Isoforms :

All SWI/SNF Complex Isoforms :

In Vitro

AU-24118 (3, 10, 30 nM; 4 h) efficiently degrades SMARCA4 and PBRM1 in VCaP prostate cancer cells^[1].
AU-24118 (100 nM; 2 h) selectively degrades SMARCA2, SMARCA4 and PBRM1 in VCaP prostate cancer cells, with no significant off-target degradation of other bromodomain-containing proteins or non-targeted mSWI/SNF subunits^[1].
AU-24118 (administered for 5 days) potently inhibits the viability of transcription factor-dependent cancer cell lines (VCaP, 22Rv1, LNCaP, C4-2B), with IC₅₀ values ranging from ~3 nM to ~30 nM; in contrast, non-transcription factor-driven cancer cell lines and normal cell lines (HEK293, PANC-1, MIA PaCa-2) are resistant to it, with IC₅₀ values > 100 nM^[1].
AU-24118 (1.5-6 μM; 5 days) exerts selective activity against PBRM1^−/− human colorectal cancer cell line HCT116, with an IC₅₀ of 1.179 μM and a selectivity index of 3.2, but shows no genotype-specific activity in PBRM1^−/− MC38 or B16F10 cells^[2].
AU-24118 (0.75-6 μM; 12 days) exerts comparable inhibitory effects on clonogenic survival in wild-type and PBRM1^−/− human colorectal cancer cell line HCT116, with no genotype-specific activity^[2].
AU-24118 (administered continuously for 5 days) potently and selectively inhibits the proliferation of SCLC-P cell lines, with IC₅₀ values ranging from 3.01 to 20.59 nM, while it exhibits only extremely low activity against SCLC-A, SCLC-N and SCLC-Y cell lines^[3].
Treatment of PBRM1^+/+ and PBRM1^−/− HCT116 cells with AU-24118 (0-6 μM; 24 h) induces no significant genotype-selective cell cycle changes^[2].
AU-24118 (administered for 5 consecutive days) potently inhibits the viability of most human myeloma cell lines, with a median IC₅₀ of 5.9 nM. It shows a trend of enhanced activity in t (4;14)-positive subtypes and exhibits picomolar potency in sensitive cell lines^[4].

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

Western Blot Analysis^[1]

Cell Line:

VCaP prostate cancer cells
Concentration:

3, 10, 30 nM
Incubation Time:

4 h
Result:

Induced concentration-dependent degradation of SMARCA4 and PBRM1.

Cell Viability Assay^[2]

Cell Line:

HCT116 PBRM1+/+ and PBRM1−/−; MC38 PBRM1+/+ and PBRM1−/−; B16F10 PBRM1+/+ and PBRM1−/−
Concentration:

0, 1.5, 3, 6 μM
Incubation Time:

5 days
Result:

Preferentially reduced HCT116 PBRM1−/− cell viability, with IC50 values of 1.179 μM in PBRM1−/− cells and 3.880 μM in PBRM1+/+ cells, but showed no PBRM1-loss selectivity in MC38 or B16F10 cells.

Western Blot Analysis^[3]

Cell Line:

NCI-H1048; NCI-H526
Concentration:

3, 10, 30, 100, 1000 nM
Incubation Time:

4 h
Result:

Dose-dependently degraded SMARCA4 and PBRM1 and reduced POU2F3, with marked effects at ≥30 nM.

Western Blot Analysis^[3]

Cell Line:

NCI-H1048; NCI-H526
Concentration:

30 nM
Incubation Time:

1, 2, 4, 8, 12, 16, 24 h
Result:

Progressively reduced SMARCA4, PBRM1, and POU2F3 protein levels over time.

Parmacokinetics

Species	Dose	Route	AUC_0-last	T_max
Mice^[1]	30 mg/kg	p.o.	14716 ng·h/mL	3 h
Mice^[1]	10 mg/kg	p.o.	4929 ng·h/mL	6 h
Mice^[1]	100 mg/kg	p.o.	32178 ng·h/mL	4 h

In Vivo

AU-24118 (15 mg/kg; p.o.; three times weekly; 4 weeks) induces complete regression of all VCaP CRPC xenograft tumors, with robust degradation of target proteins, inhibition of oncogenic markers, and induction of apoptosis^[1].
AU-24118 (15-20 mg/kg; p.o.; three times weekly; 25 days) has a maximum tolerated dose of 15 mg/kg (p.o., three times weekly) in tumor-free CB17 SCID mice, with minimal toxicity to host organs and only a slight elevation in ALT after prolonged treatment^[1].
AU-24118 (1.875-7.5 mg/kg) causes early mortality and rapid body weight loss in hCRBN transgenic mice at doses ≥1.875 mg/kg^[4].
AU-24118 (15 mg/kg; p.o.; three times weekly) enhances the anti-tumor efficacy of cisplatin plus etoposide in NCI-H526 SCLC-P xenografts, but concurrent administration causes body weight loss^[3].
AU-24118 (15 mg/kg; p.o.; three times weekly; 2 weeks) demonstrates potent anti-tumor efficacy against SCLC-P patient-derived xenografts with no signs of toxicity^[3].
AU-24118 (15 mg/kg; p.o.; three times weekly; 3-4 weeks) exhibits potent anti-tumor efficacy against multiple myeloma subcutaneous xenografts, with greater activity than standard-of-care agents pomalidomide and carfilzomib, and no signs of single-agent toxicity^[3].
AU-24118 (1 mg/kg; three times per week; 2 weeks) achieves a 40% reduction in serum M-protein in de novo Vk*MYC^hCRBN multiple myeloma mice with good tolerability^[4].
AU-24118 (15 mg/kg; p.o.; three times weekly; until study endpoint) potently inhibits tumor proliferation and extends survival in a disseminated multiple myeloma orthotopic xenograft model, with complete abatement of tumor cells observed in marrow tissue^[3].

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

Animal Model:

CB17 severe combined immunodeficiency (SCID) (male, 6 weeks old, subcutaneous xenograft of VCaP cells, castrated post-tumor growth)^[1]
Dosage:

15 mg/kg
Administration:

p.o.; three times weekly; 4 weeks
Result:

Induced regression in every tumor, with individual tumors showing a decrease in volume from baseline (endpoint waterfall plot values below 0%).
Robustly downregulated SMARCA2, SMARCA4, PBRM1, AR, ERG, c-Myc, and PSA, along with increased cleaved PARP levels in day 5 tumors via western blot analysis.
Revealed increased apoptosis via TUNEL staining.
Confirmed SMARCA4 degradation, downregulation of AR, ERG, c-Myc, and reduced Ki-67 proliferation marker levels via IHC.
Caused no significant body weight changes during treatment.

Animal Model:

CB17 severe combined immunodeficiency (SCID) (male)^[1]
Dosage:

15 mg/kg; 20 mg/kg
Administration:

p.o.; three times weekly; 25 days
Result:

Caused noticeable weight loss after 1 week, with morbidity or fatality by week 2 in mice receiving 20 mg/kg.
Allowed all mice receiving up to 15 mg/kg to tolerate treatment well.
Showed no discernible toxicity in spleen, kidney, and liver via H&E staining after 15 mg/kg treatment.
Confirmed successful target degradation in normal tissues via immunohistochemistry.
Resulted in only a slight elevation in alanine transaminases (ALT), with all other blood panel values comparable to vehicle-treated mice and within normal ranges after 25 days of 15 mg/kg treatment.

Animal Model:

CB17/lcr-Prkdcscid/IcrlcoCrl (SCID) (gender matched to cell line donor, 6 weeks old)^[3]
Dosage:

15 mg/kg
Administration:

p.o.; three times weekly; 3-4 weeks
Result:

Caused significant reductions in SCLC-P (NCI-H526 and NCI-H1048) tumor volumes and weights.
Showed no significant effect on SCLC-A (NCI-H69) tumor growth.
Induced degradation of SMARCA2, SMARCA4, and PBRM1, downregulation of POU2F3, POU2AF2, GFI1B, and N-MYC, and increased cleaved PARP in SCLC-P tumors.
Revealed increased apoptotic bodies, necrotic debris, and TUNEL-positive cells in SCLC-P tumors via histopathological analysis.
Demonstrated loss of SMARCA4, POU2F3, and tuft cell marker DCLK1 in SCLC-P tumors via IHC.
Caused no significant changes in body weight or DCLK1-positive tuft cells in normal lung and small intestine tissues.

Animal Model:

CB17/lcr-Prkdcscid/IcrlcoCrl (SCID) (gender matched to cell line donor, 6 weeks old)^[3]
Dosage:

15 mg/kg
Administration:

p.o.; three times weekly
Result:

Showed enhanced tumor growth inhibition when combined with cisplatin and etoposide compared to AU-24118 or chemotherapy alone, despite chemotherapy being stopped at day 8.
Led to 10-20% body weight loss in the combination group, while no weight loss was observed in the AU-24118 single-agent group.

Animal Model:

NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (6-8 weeks old)^[3]
Dosage:

15 mg/kg
Administration:

p.o.; three times weekly; 2 weeks
Result:

Significantly inhibited Lx1322 tumor growth without causing changes in body weight.
Induced degradation of SMARCA2, SMARCA4, and PBRM1, and loss of SMARCA4 protein expression via IHC in tumors.

Animal Model:

CB17/lcr-Prkdcscid/IcrlcoCrl (SCID) (gender matched to cell line donor, 6 weeks old)^[3]
Dosage:

15 mg/kg
Administration:

p.o.; three times weekly; 3-4 weeks
Result:

Significantly decreased tumor volumes and weights in MM1.S, NCI-H929, and Karpas-25 xenograft models.
Achieved complete tumor regression in all MM1.S-treated mice.
Induced degradation of SMARCA2, SMARCA4, and PBRM1, downregulation of c-MYC and POU2AF1, and loss of SMARCA4 and c-MYC protein expression via IHC in MM1.S tumors.
Caused no notable changes in body weight.

Animal Model:

CB17/lcr-Prkdcscid/IcrlcoCrl (SCID) (gender matched to cell line donor, 6 weeks old)^[3]
Dosage:

15 mg/kg
Administration:

p.o.; three times weekly; until study endpoint
Result:

Caused a substantial reduction in bioluminescence signal over time and at endpoint, indicating diminished tumor proliferation.
Significantly extended overall survival of treated mice.
Induced a significant increase in apoptotic cells via TUNEL staining, and confirmed loss of SMARCA4 and c-MYC in treated tumors via IHC.
Revealed near-total absence of plasma cells (tumor cells) in treated marrow, with remnant hematopoietic cells and RBC-filled sinusoids indicative of tumor regression via histopathological analysis.

Animal Model:

Vk*MYC^hCRBN (hCRBN-expressing, de novo multiple myeloma model)^[4]
Dosage:

1 mg/kg
Administration:

three times per week; 2 weeks
Result:

Reduced serum M-protein by approximately 40% within 2 weeks.
Caused no notable weight loss.

Chemical Information

CAS No. 3084244-26-5
Appearance Solid
분자량 632.75
화학식 C₃₇H₄₀N₆O₄
Color Light yellow to brown
SMILES

NC1=C(C=C(N=N1)C2=C(C=CC=C2)O)C3=CC=C(C=C3)N4CCC(CC4)N5CCC(CC5)C6=CC=C(C=C6)OC7CCC(NC7=O)=O
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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Cell

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

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

2025 April 16.

용액&용해도

In Vitro:

DMSO : 8.33 mg/mL (13.16 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)

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

1.5804 mL

7.9020 mL

15.8040 mL

5 mM

0.3161 mL

1.5804 mL

3.1608 mL

10 mM

0.1580 mL

0.7902 mL

1.5804 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 0.83 mg/mL (1.31 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (1.31 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (1.31 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 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 (8.3 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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: 12.5 mg/mL (19.76 mM); Suspended solution; Need ultrasonic

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (291 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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)

References

[1]. He T, et al. Development of an orally bioavailable mSWI/SNF ATPase degrader and acquired mechanisms of resistance in prostate cancer. Proceedings of the National Academy of Sciences of the United States of America. 2024 Apr 09;121(15):e2322563121. [Content Brief]

[2]. Islam MT, et al. Synthetic lethality between PBRM1 deficiency and PARP inhibitors: exploiting G2/M checkpoint arrest in colorectal cancer. Molecular medicine (Cambridge, Mass.). 2026 Jun 06. [Content Brief]

[3]. He T, et al. Targeting the mSWI/SNF complex in POU2F-POU2AF transcription factor-driven malignancies. Cancer cell. 2024 Aug 12;42(8):1336-1351.e9. [Content Brief]

[4]. Yamashita Y, et al. Preclinical evaluation of SWI/SNF targeting agents in multiple myeloma including t(4;14) subtypes. Blood. 2025;146(Suppl 1):2138-2139.

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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.5804 mL	7.9020 mL	15.8040 mL	39.5101 mL
	5 mM	0.3161 mL	1.5804 mL	3.1608 mL	7.9020 mL
	10 mM	0.1580 mL	0.7902 mL	1.5804 mL	3.9510 mL

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AU-24118

Publications Citing Use of MedChemExpress (MCE) AU-24118

All PROTACs Isoforms

All SWI/SNF Complex Isoforms