Cat. No.: HY-179433

PROTAC AR Degrader-12

Name: PROTAC AR Degrader-12
Brand: MedChemExpress
SKU: HY-179433
Price: 1050.00 USD
Availability: InStock
Rating: 5 (1 reviews)

고객리뷰

Based on 1 Customer Validation

PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer.
(Pink: AR ligand (HY-179442); Blue: VHL ligand (HY-112078); Black: linker).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity : 98.52%
화학식: C₅₇H₇₆N₈O₁₀S
분자량:1065.33

보관:

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

PROTAC AR Degrader-12 Chemical Structure

사이즈

가격

재고

수량

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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
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer^[1]. (Pink: AR ligand (HY-179442); Blue: VHL ligand (HY-112078); Black: linker).

IC₅₀ & Target

ERα

All PROTACs Isoforms :

All Estrogen Receptor/ERR Isoforms :

All Src Isoforms :

In Vitro

PROTAC AR Degrader-12 (Compound 18o) shows good inhibitory activity against MCF-7 (IC₅₀ = 0.13 μM) and LCC2 cells(IC₅₀ = 0.54 μM) and exhibits broad-spectrum efficacy against clinically relevant mutant variants, demonstrating potent submicromolar inhibition of MCF-7^D538G(IC₅₀ = 0.66 μM), MCF-7^Y537S (IC₅₀ = 0.44 μM), and MCF-7^EGFR(IC₅₀ =0.52 μM)^[1].
PROTAC AR Degrader-12 (0.01-2 μM, 24 h) effectively and in a dose-dependent manner degrades AR protein in MCF-7 cells (DC₅₀ = 0.72 μM)^[1].
PROTAC AR Degrader-12 (1 μM, 0-24 h) shows a time-dependent effect on AR degradation in MCF-7 cells^[1].
PROTAC AR Degrader-12 (0.01-2 μM, 24 h) causes a concentration-dependent downregulation of ERα protein in MCF-7 cells^[1].
PROTAC AR Degrader-12 (0.01-2 μM, 12-24 h) significantly downregulates ERα protein in MCF-7D538G, MCF-7Y537S, MCF-7EGFR, LCC2, and T47D cells, and fails to downregulate ERβ protein in PC9 cells^[1].
PROTAC AR Degrader-12 (1 μM, 24 h) induces a decrease in ERα through an indirect mechanism, rather than by directly targeting the degradation of CBS in MCF-7 cells^[1].
PROTAC AR Degrader-12 (0-5 μM, 0-24 h) reduces AR protein in MCF-7 cells due to posttranscriptional degradation, while the reduction in ERα was a result of transcriptional repression^[1].
PROTAC AR Degrader-12 exhibits potent antiproliferative activity in AR-overexpressing but ERα-deficient prostate cancer cells LNCaP (IC₅₀ = 0.46 μM), while its antiproliferative activity is significantly reduced in AR-negative MDA-MB-231 cells (IC₅₀ > 30 μM)^[1].
PROTAC AR Degrader-12 was very effective in stabilizing the AR protein at high temperature, while it only displays a weak protective effect on ERα protein, suggesting that compound PROTAC AR Degrader-12 engages AR but does not bind to Erα in LCC2 cells^[1].
PROTAC AR Degrader-12 (1 μM, 24 h) significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1 in MCF-7 cells^[1].
PROTAC AR Degrader-12 (1-10 μM, 48 h) induces S-phase cell cycle arrest in MCF-7 and LCC2 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

MCF-7 cells
Concentration:

0.01 μM, 0.1 μM, 1 μM, 2 μM
Incubation Time:

0 h, 3 h, 6 h, 12 h, 18 h, 24 h
Result:

Effectively and in a dose-dependent manner degraded AR protein.
Time-dependent effect on AR degradation.
Caused a concentration-dependent downregulation of ERα protein.

Real Time qPCR^[1]

Cell Line:

MCF-7 cells
Concentration:

0 μM, 1 μM, 5 μM
Incubation Time:

0 h, 4 h, 24 h
Result:

AR mRNA expression increased significantly with increasing concentration; ERα mRNA expression was downregulated.
The expression of ERα target genes (TFF1, PGR) and AR target genes (PSA, TMPRSS2) was significantly suppressed after 24 hours.
Significantly inhibited the mRNA expression of FOXA1, GREB1, SRC, and PELP1.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	CL	MRT_0-t	MRT_0-∞	F
Rat	2 mg/kg	i.v.	28.5 h	0.11 h	639.02 ng/mL	514 ng·h/mL	545.39 ng·h/mL	760.12 mL/h/kg	2.97 h	10.20 h	/
Rat	20 mg/kg	p.o.	38.53 h	1.08 h	2.69 ng/mL	43.70 ng·h/mL	105.74 ng·h/mL	40313.87 mL/h/kg	20.92 h	89.95 h	1.94 %
Rat	4 mg/kg	i.p.	14.18 h	0.39 h	31.19 ng/mL	85.74 ng·h/mL	91.28 ng·h/mL	8800.82 mL/h/kg	12.13 h	15.52 h	16.74 %

In Vivo

PROTAC AR Degrader-12 (Compound 18o) (5-10 μM/kg, i.p., once every other day) significantly inhibits tumor growth in MCF-7 cells and LCC2 cells xenograft mice, promotes AR protein degradation and ERα signaling inhibition, without weight loss or other toxicities^[1].

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

Animal Model:

Balb/c nude mice (female, 4 weeks old) were subcutaneously injected with MCF-7 human breast cancer cells (5 × 10⁶ cells)^[1].
Dosage:

5 μM/kg, 10 μM/kg
Administration:

I.p., once every other day
Result:

At a dose of 10 μM/kg, it significantly inhibited tumor growth.
Tumor volume decreased, and Ki67 proliferation marker expression was reduced.
AR and ERα protein levels were downregulated in tumor tissue.
No significant change in body weight or significant toxicity was observed.

Animal Model:

Balb/c nude mice (female, 4 weeks old) were subcutaneously injected with tamoxifen-resistant LCC2 human breast cancer cells (5 × 10⁶ cells)^[1].
Dosage:

5 μM/kg, 10 μM/kg
Administration:

I.p., once every other day
Result:

Tumor growth inhibition rate (TGI) reached 58% at a dose of 10 μM/kg.
Ki67 expression was decreased, and AR and ERα proteins were downregulated.
Body weight remained stable, with no signs of toxicity.

Related Protocols :

Chemical Information

Appearance Solid
분자량 1065.33
화학식 C₅₇H₇₆N₈O₁₀S
Color Off-white to light yellow
SMILES

CC(COC1=C(C=CC(C(N2CCC(CN3CCCC(C(N[C@@H](C(C)(C)C)C(N4[C@H](C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)C[C@@H](O)C4)=O)=O)C3)CC2)=O)=C1)NC(C7=CC(OCC(C)C)=C(C=C7)[N+]([O-])=O)=O)C
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

용액&용해도

In Vitro:

DMSO : 100 mg/mL (93.87 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

0.9387 mL

4.6934 mL

9.3868 mL

5 mM

0.1877 mL

0.9387 mL

1.8774 mL

10 mM

0.0939 mL

0.4693 mL

0.9387 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 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (2.35 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Wu Y, et al. Kill Two Birds with One Stone: An Efficient and Potent AR CBS-Targeted Degrader Reverses Breast Cancer Resistance via Concurrent AR Degradation and ERα Transcriptional Suppression. J Med Chem. 2025 Nov 27;68(22):24136-24167. [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

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	0.9387 mL	4.6934 mL	9.3868 mL	23.4669 mL
	5 mM	0.1877 mL	0.9387 mL	1.8774 mL	4.6934 mL
	10 mM	0.0939 mL	0.4693 mL	0.9387 mL	2.3467 mL
	15 mM	0.0626 mL	0.3129 mL	0.6258 mL	1.5645 mL
	20 mM	0.0469 mL	0.2347 mL	0.4693 mL	1.1733 mL
	25 mM	0.0375 mL	0.1877 mL	0.3755 mL	0.9387 mL
	30 mM	0.0313 mL	0.1564 mL	0.3129 mL	0.7822 mL
	40 mM	0.0235 mL	0.1173 mL	0.2347 mL	0.5867 mL
	50 mM	0.0188 mL	0.0939 mL	0.1877 mL	0.4693 mL
	60 mM	0.0156 mL	0.0782 mL	0.1564 mL	0.3911 mL
	80 mM	0.0117 mL	0.0587 mL	0.1173 mL	0.2933 mL

상품명:
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PROTAC AR Degrader-12

All PROTACs Isoforms

All Estrogen Receptor/ERR Isoforms

All Src Isoforms