2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. EN1441

EN1441 is a covalent degrader targeting the androgen receptor (AR) with an EC50 value of 4.2 μM and its truncated variant AR-V7. EN1441 selectively and potently degrades both AR and AR-V7 in androgen-independent prostate cancer cells. EN1441 is promising for research of androgen-independent prostate cancers.

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

EN1441 Chemical Structure

EN1441 Chemical Structure

CAS No. : 2196448-47-0

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Based on 1 publication(s) in Google Scholar

EN1441 Related Antibodies

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Description

EN1441 is a covalent degrader targeting the androgen receptor (AR) with an EC50 value of 4.2 μM and its truncated variant AR-V7. EN1441 selectively and potently degrades both AR and AR-V7 in androgen-independent prostate cancer cells. EN1441 is promising for research of androgen-independent prostate cancers[1].

In Vitro

EN1441 (0.1-50 μM; 1-24 h) shows dose-responsive degradation of AR and AR-V7 with rapid loss occurring at one hour[1].
EN1441 (0.1-100 μM) EN1441 completely inhibits total AR transcriptional activity in androgen-independent prostate cancer cells expressing both AR and AR-V7[1].
EN1441 selectively degrades AR and AR-V7 in a proteasome-dependent manner through direct covalent targeting of an intrinsically disordered cysteine C125 in AR and AR-V7. EN1441 causes significant and selective destabilization of AR and AR-V7, leading to aggregation of AR/AR-V7 and subsequent proteasome-mediated degradation[1].

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

EN1441 Related Antibodies

Western Blot Analysis[1]

Cell Line: 22Rv1 cells
Concentration: 0.1 μM, 1 μM, 10 μM, 50 μM
Incubation Time: 1 h, 3 h, 6 h, 9 h, 12 h, 24 h
Result: Showed dose-responsive degradation of AR and AR-V7 with rapid loss occurring at one hour.
Molecular Weight

264.71

Formula

C13H13ClN2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC2=C(NC(C(N2C(C=C)=O)(C)C)=O)C=C1
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 : 125 mg/mL (472.21 mM; Need ultrasonic; 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 3.7777 mL 18.8886 mL 37.7772 mL
5 mM 0.7555 mL 3.7777 mL 7.5554 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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C1

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Volume (start)

V1

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C2

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V2

In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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 3.7777 mL 18.8886 mL 37.7772 mL 94.4430 mL
5 mM 0.7555 mL 3.7777 mL 7.5554 mL 18.8886 mL
10 mM 0.3778 mL 1.8889 mL 3.7777 mL 9.4443 mL
15 mM 0.2518 mL 1.2592 mL 2.5185 mL 6.2962 mL
20 mM 0.1889 mL 0.9444 mL 1.8889 mL 4.7221 mL
25 mM 0.1511 mL 0.7555 mL 1.5111 mL 3.7777 mL
30 mM 0.1259 mL 0.6296 mL 1.2592 mL 3.1481 mL
40 mM 0.0944 mL 0.4722 mL 0.9444 mL 2.3611 mL
50 mM 0.0756 mL 0.3778 mL 0.7555 mL 1.8889 mL
60 mM 0.0630 mL 0.3148 mL 0.6296 mL 1.5740 mL
80 mM 0.0472 mL 0.2361 mL 0.4722 mL 1.1805 mL
100 mM 0.0378 mL 0.1889 mL 0.3778 mL 0.9444 mL
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EN1441 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:

EN14412196448-47-0EN 1441EN-1441Androgen ReceptorARAR-V7prostate cancerInhibitorinhibitorinhibit

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