2. PROTAC Vitamin D Related/Nuclear Receptor
  3. Ligands for E3 Ligase Ligands for Target Protein for PROTAC Androgen Receptor
  4. AR antagonist 1 hydrochloride

AR antagonist 1 hydrochloride 

Cat. No.: HY-130845A Purity: 99.53%
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AR antagonist 1 (compound 29) hydrochloride is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).

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

AR antagonist 1 hydrochloride Chemical Structure

AR antagonist 1 hydrochloride Chemical Structure

CAS No. : 1818885-55-0

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Based on 1 publication(s) in Google Scholar

Other Forms of AR antagonist 1 hydrochloride:

AR antagonist 1 hydrochloride Related Antibodies

Top Publications Citing Use of Products

View All Ligands for E3 Ligase Isoform Specific Products:

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von Hippel-Lindau (VHL) MDM2 Cereblon IAP

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Description

AR antagonist 1 (compound 29) hydrochloride is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020)[1].

In Vitro

AR antagonist 1 (compound 29) hydrochloride is the ligand for target ligase of ARD-266. ARD-266 is a highly potent and VHL E3 ligase-based?androgen receptor (AR)?PROTAC degrader[1].
AR antagonist 1 exhibits micromolar binding affinity to its E3 ligase complex, it can be successfully employed for the design of highly potent and efficient PROTAC degraders[1].
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein.
PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

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

AR antagonist 1 hydrochloride Related Antibodies
Molecular Weight

315.24

Formula

C15H20Cl2N2O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

[H]Cl.N#CC1=CC=C(O[C@H]2C(C)(C)[C@H](N)C2(C)C)C=C1Cl
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 : 62.5 mg/mL (198.26 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 3.1722 mL 15.8609 mL 31.7219 mL
5 mM 0.6344 mL 3.1722 mL 6.3444 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.

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

Mass
=
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

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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 3.1722 mL 15.8609 mL 31.7219 mL 79.3047 mL
5 mM 0.6344 mL 3.1722 mL 6.3444 mL 15.8609 mL
10 mM 0.3172 mL 1.5861 mL 3.1722 mL 7.9305 mL
15 mM 0.2115 mL 1.0574 mL 2.1148 mL 5.2870 mL
20 mM 0.1586 mL 0.7930 mL 1.5861 mL 3.9652 mL
25 mM 0.1269 mL 0.6344 mL 1.2689 mL 3.1722 mL
30 mM 0.1057 mL 0.5287 mL 1.0574 mL 2.6435 mL
40 mM 0.0793 mL 0.3965 mL 0.7930 mL 1.9826 mL
50 mM 0.0634 mL 0.3172 mL 0.6344 mL 1.5861 mL
60 mM 0.0529 mL 0.2643 mL 0.5287 mL 1.3217 mL
80 mM 0.0397 mL 0.1983 mL 0.3965 mL 0.9913 mL
100 mM 0.0317 mL 0.1586 mL 0.3172 mL 0.7930 mL
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AR antagonist 1 hydrochloride 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:

AR antagonist 11818885-55-0AR antagonist1AR antagonist-1Ligands for E3 LigaseLigands for Target Protein for PROTACAndrogen ReceptorE3 ligase-recruiting MoietyTarget Protein-binding MoietyPROTACLinkertumorcancerLNCaPVCaPInhibitorinhibitorinhibit

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