EST1140
EST1140 is a covalent molecular glue degrader targeting RNF126 for AR/AR-V7, with DC50 values of 33 μM and 30 μM, respectively, in 22Rv1 cells. EST1140 covalently binds to the E3 ligase RNF126 to achieve targeted protein degradation. EST1140 can be used in the research of androgen-independent prostate cancer.
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- CAS No.: 3105892-11-0
- Formule: C30H32N4O6S
- Masse moléculaire:576.66
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Help & FAQs
Activité biologique
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AR-V7 |
RNF126 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 22Rv1 | DC50 |
33 μM
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50% degradation concentration of AR in human 22Rv1 androgen-independent prostate cancer cells after 24 h of treatment, assessed by Western blot assay.
50% degradation concentration of AR in human 22Rv1 androgen-independent prostate cancer cells after 24 h of treatment, assessed by Western blot assay.
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41867716 |
| 22Rv1 | DC50 |
30 μM
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50% degradation concentration of AR-V7 in human 22Rv1 androgen-independent prostate cancer cells after 24 h of treatment, assessed by Western blot assay.
50% degradation concentration of AR-V7 in human 22Rv1 androgen-independent prostate cancer cells after 24 h of treatment, assessed by Western blot assay.
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41867716 |
| 22Rv1 | EC50 |
8 μM
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Half-maximal effective concentration for inhibition of AR/AR-V7 transcriptional activity in human 22Rv1 androgen-independent prostate cancer cells after 12 h of treatment, assessed by luciferase reporter assay.
Half-maximal effective concentration for inhibition of AR/AR-V7 transcriptional activity in human 22Rv1 androgen-independent prostate cancer cells after 12 h of treatment, assessed by luciferase reporter assay.
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41867716 |
EST1140 (20 μM; 24 h)-mediated degradation of AR-V7 in 22Rv1 cells is dependent on the proteasome[1].
Treatment with EST1140 (1-50 μM; 24 h) for 24 h induces dose-dependent degradation of AR (DC50 = 33 μM) and AR-V7 (DC50 = 30 μM) in 22Rv1 androgen-independent prostate cancer cells[1].
EST1140 (8 μM; 12 h) potently inhibits the transcriptional activity of AR/AR-V7 in 22Rv1 cells, with an EC50 of 8 μM[1].
EST1140 (0.1-50 μM; 30 min) covalently binds to purified RNF126 protein in a dose-dependent manner in IA-rhodamine-labeled competition assays[1].
The effect of EST1140 (20 μM; 24 h) on inducing FLAG-AR degradation in HEK293T cells is strictly dependent on RNF126[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:22Rv1 androgen-independent prostate cancer cells
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Concentration:20 μM
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Incubation Time:24 h
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Result:Mediated degradation of AR-V7, which was attenuated by pre-treatment with proteasome inhibitor.
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Cell Line:22Rv1 androgen-independent prostate cancer cells
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Concentration:1, 5, 10, 20, 35, 50 μM
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Incubation Time:24 h
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Result:Induced dose-dependent degradation of both AR and AR-V7.
Achieved a 50% degradation concentration (DC50) of 33 μM for AR.
Achieved a 50% degradation concentration (DC50) of 30 μM for AR-V7.
Caused observable degradation as early as 4 h after treatment.
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Cell Line:FLAG-AR-expressing RNF126 wild-type (WT) and knockout (KO) HEK293T cells
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Concentration:20 μM
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Incubation Time:24 h
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Result:Significantly reduced FLAG-AR levels in RNF126 WT cells.
Abrogated FLAG-AR degradation in RNF126 KO cells.
Chemical Information
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CAS No. 3105892-11-0
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Masse moléculaire 576.66
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Formule C30H32N4O6S
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SMILES
COC1=CC=C(C(/C=C/C(N[C@@H]2C[C@@H](NC(COC3=CC=C(C4=CSC(N5CCOCC5)=N4)C=C3)=O)C2)=O)=O)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EST1140 Related Classifications
HY-187458 Related Classifications
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