2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. AU-24118

AU-24118 is a selective and orally bioavailable PROTAC degrader of mSWI-SNF ATPases (SMARCA2 and SMARCA4) and PBRM1. AU-24118 integrates a bait moiety binding to the bromodomains of SMARCA2 and SMARCA4, along with a ligand moiety for CRBN ligase. AU-24118 demonstrates tumor regression in prostate cancer model. AU-24118 can be studied to combat prostate cancer. (Pink: PBRM1/SMARCA2,4 ligand (HY-171774); Blue: CRBN ligand (HY-171775)).

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AU-24118 Chemical Structure

AU-24118 Chemical Structure

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Based on 1 publication(s) in Google Scholar

AU-24118 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

AU-24118 is a selective and orally bioavailable PROTAC degrader of mSWI-SNF ATPases (SMARCA2 and SMARCA4) and PBRM1. AU-24118 integrates a bait moiety binding to the bromodomains of SMARCA2 and SMARCA4, along with a ligand moiety for CRBN ligase. AU-24118 demonstrates tumor regression in prostate cancer model. AU-24118 can be studied to combat prostate cancer. (Pink: PBRM1/SMARCA2,4 ligand (HY-171774); Blue: CRBN ligand (HY-171775))[1].

In Vitro

AU-24118 (3-30 nM, 4 h) demonstrates comparable degradation efficacy of SMARCA4 and PBRM1 in VCaP prostate cancer cells[1].
AU-24118 (1 μM, 2 h) selectively degrades SMARCA2, SMARCA4, and PBRM1, resulting in their significant downregulation in VCaP cells[1].
AU-24118 (0.1 μM, 4 h) degrades SMARCA2 and PBRM1 in AUR-1 and AUR-2 cells, but is unable to degrade SMARCA4 in AUR-2 cells[1].

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

AU-24118 Related Antibodies

Western Blot Analysis[1]

Cell Line: VCaP cell line-derived xenograft model
Concentration: 15 mg/kg
Incubation Time: 5 d
Result: Downregulated SMARCA2, SMARCA4 and PBRM1 as well as specific prostate cancer lineage proteins (AR, ERG, C-Myc, and PSA) after 5 day with AU-24118 alone or with Enzalutamide (HY-70002).
Parmacokinetics
Species Dose Route Indicator value
Mice 10 mg/kg p.o. AUC0-t 4929 ng·h/mL
Mice 100 mg/kg p.o. Tmax 4 hr
Mice 30 mg/kg p.o. AUC0-t 14716 ng·h/mL
Mice 10 mg/kg p.o. Tmax 6 hr
Mice 100 mg/kg p.o. AUC0-t 32178 ng·h/mL
Mice 30 mg/kg p.o. Tmax 3 hr
In Vivo

AU-24118 (15 mg/kg, p.o., 3 days per week) leads to tumor regression in CB17 SCID mice and results in better effect when combined with Enzalutamide (HY-70002) (10 mg/kg, p.o., 5 times per week), rendering some tumors unpalpable[1].

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

Animal Model: Six-week-old CB17 (male) SCID mice injected with 3 x 106 VCaP cells (s.c.) into the dorsal flank on both sides in a 1:1 mixture of serum free medium[1]
Dosage: 15 mg/kg
Administration: Oral gavage (p.o.), 3 times per week
Result: Downregulated SMARCA2, SMARCA4, and PBRM1 and specific prostate cancer lineage proteins including AR, ERG, C-Myc and Ki-67.
Induced apoptosis as evidenced by increased cleaved PARP levels.
Did not lead to significant body weight changes, indicating the mice tolerated AU-24118 with or without the addition of Enzalutamide.
Molecular Weight

632.75

Formula

C37H40N6O4
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5804 mL 7.9020 mL 15.8040 mL
5 mM 0.3161 mL 1.5804 mL 3.1608 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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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: ≥ 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.

    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: ≥ 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.

    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.

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

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).
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

Purity: 99.10%

SDS (251 KB)

COA (244 KB) HNMR (142 KB) RP-HPLC (165 KB) LCMS (436 KB)

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, 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 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-24118AU24118AU 24118PROTACsEpigenetic Reader DomainPROTACcancercastration-resistant prostate cancer (CRPC)Inhibitorinhibitorinhibit

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