2. PROTAC Vitamin D Related/Nuclear Receptor Protein Tyrosine Kinase/RTK
  3. PROTACs Androgen Receptor Estrogen Receptor/ERR Src
  4. PROTAC AR Degrader-12

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).

For research use only. We do not sell to patients.

PROTAC AR Degrader-12

PROTAC AR Degrader-12 Chemical Structure

Size Price Stock Quantity
5 mg Get quote 8 - 10 Weeks 7 - 9 Weeks 9 - 11 Weeks 8 - 10 weeks
10 mg Get quote 8 - 10 Weeks 7 - 9 Weeks 9 - 11 Weeks 8 - 10 weeks
25 mg Get quote 8 - 10 Weeks 7 - 9 Weeks 9 - 11 Weeks 8 - 10 weeks
50 mg Get quote 8 - 10 Weeks 7 - 9 Weeks 9 - 11 Weeks 8 - 10 weeks
100 mg Get quote 8 - 10 Weeks 7 - 9 Weeks 9 - 11 Weeks 8 - 10 weeks
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PROTAC AR Degrader-12 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

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Lck Fyn Blk Fgr Hck Lyn Yes SRC-3

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Description

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

 

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-7D538G(IC50 = 0.66 μM), MCF-7Y537S (IC50 = 0.44 μM), and MCF-7EGFR(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.

PROTAC AR Degrader-12 Related Antibodies

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 T1/2 Tmax Cmax AUC0-t AUC0-∞ CL MRT0-t MRT0-∞ 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.
Molecular Weight

1065.33

Formula

C57H76N8O10S
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC AR Degrader-12 Related Classifications

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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:

PROTAC AR Degrader-12PROTAC AR Degrader12PROTAC AR Degrader 12PROTACsAndrogen ReceptorEstrogen Receptor/ERRSrcPROTACAREndocrine ResistanceBreast CancerInhibitorinhibitorinhibit

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