2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. RD162

RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer.

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

RD162 Chemical Structure

RD162 Chemical Structure

CAS No. : 915087-27-3

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Based on 1 publication(s) in Google Scholar

RD162 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer[1].

In Vitro

RD162 (1-10 μM; 4 days) suppresses growth and induces apoptosis in the human prostate cancer cell line VCaP which has endogenous AR gene amplification[1].
RD162 has little to no binding to the progesterone, estrogen or glucocorticoid receptors in an in vitro fluorescence polarization assay[1].

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

RD162 Related Antibodies

Cell Viability Assay[1]

Cell Line: VCaP cells
Concentration: 1, 10 μM
Incubation Time: 4 days
Result: Suppressed cell growth.
In Vivo

RD162 (10 mg/kg; oral gavage; daily; for 28 days) causes all tumors regressed[1].
RD162 (0.1, 1, 10 mg/kg; oral gavage; daily; for 5 days) consistently reduces luciferase activity with 10 mg/kg/day human LNCaP/AR xenografts grown in castrated male mice whereas lower doses of 0.1 and 1.0 mg/kg/day has minimal effect. RD162 substantially reduces cellular proliferation after 5 days[1].
RD162 (20 mg/kg; gavage) is ∼50 percent bioavailable after oral delivery with a serum half-life of about 30 hours[1].

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

Animal Model: Castrate male mice bearing LNCaP/AR xenografts[1]
Dosage: 10 mg/kg
Administration: Oral gavage; daily; for 28 days
Result: Caused all tumors regressed.
Animal Model: Male mice[1]
Dosage: 20 mg/kg (Pharmacokinetic Analysis)
Administration: Oral gavage (in 0.5% hydroxy-methyl-propyl-cellulose)
Result: Had ∼50 percent bioavailable after oral delivery with a serum half-life of about 30 hours.
Molecular Weight

476.45

Formula

C22H16F4N4O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC)C1=CC=C(N(C(N(C2=CC=C(C#N)C(C(F)(F)F)=C2)C3=O)=S)C43CCC4)C=C1F
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 (262.36 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 2.0989 mL 10.4943 mL 20.9886 mL
5 mM 0.4198 mL 2.0989 mL 4.1977 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)

Mass
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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

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C2

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V2

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

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mg/kg

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g

Dosing volume
(per animal)

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Number of animals

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 2.0989 mL 10.4943 mL 20.9886 mL 52.4714 mL
5 mM 0.4198 mL 2.0989 mL 4.1977 mL 10.4943 mL
10 mM 0.2099 mL 1.0494 mL 2.0989 mL 5.2471 mL
15 mM 0.1399 mL 0.6996 mL 1.3992 mL 3.4981 mL
20 mM 0.1049 mL 0.5247 mL 1.0494 mL 2.6236 mL
25 mM 0.0840 mL 0.4198 mL 0.8395 mL 2.0989 mL
30 mM 0.0700 mL 0.3498 mL 0.6996 mL 1.7490 mL
40 mM 0.0525 mL 0.2624 mL 0.5247 mL 1.3118 mL
50 mM 0.0420 mL 0.2099 mL 0.4198 mL 1.0494 mL
60 mM 0.0350 mL 0.1749 mL 0.3498 mL 0.8745 mL
80 mM 0.0262 mL 0.1312 mL 0.2624 mL 0.6559 mL
100 mM 0.0210 mL 0.1049 mL 0.2099 mL 0.5247 mL
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RD162 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:

RD162915087-27-3RD 162RD-162Androgen ReceptordiarylthiohydantoinorallyNSAAcastrationprostateVCaPLNCaPInhibitorinhibitorinhibit

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