2. PROTAC Vitamin D Related/Nuclear Receptor
  3. PROTACs Androgen Receptor
  4. ARD-2128

ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.

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

ARD-2128 Chemical Structure

ARD-2128 Chemical Structure

CAS No. : 2222111-87-5

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1 mg USD 280 In-stock
5 mg USD 700 In-stock
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50 mg USD 3650 In-stock
100 mg USD 5900 In-stock
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Based on 1 publication(s) in Google Scholar

ARD-2128 Related Antibodies

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Description

ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer[1].

IC50 & Target

IC50: 4 nM (VCaP), 5 μM (LNCaP)[1]
In Vitro

ARD-2128 is highly potent and effective in the inhibition of cell growth in the VCaP cell line and LNCaP cell line with the IC50 values of 4 nM and 5 nM, respectively[1].
? ARD-2128 (1, 10, 100, and 1000 nM; 24 hours) effectively reduces the AR protein level by >50% at 1 nM and achieves the AR degradation of >90% at 10, 100, and 1000 nM, respectively, in VCaP cell[1].

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

ARD-2128 Related Antibodies

Cell Viability Assay[1]

Cell Line: VCaP cell
Concentration: 1, 10, 100, and 1000 nM
Incubation Time: 24 hours
Result: Reduces the AR protein level and achieves the AR degradation.
In Vivo

ARD-2128 (20 mg/kg; p.o.; once) is effective in reducing the level of AR protein in mice after 24 hours[1].
? ARD-2128 (10-40 mg/kg; p.o.; daily for 21 days) shows antitumor activity in the VCaP xenograft model in mice[1].
? ARD-2128 (5mg/kg; p.o.) treatment shows the Cmax, AUC0-t and t1/2 values of 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively[1].

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

Animal Model: SCID mice[1]
Dosage: 20 mg/kg
Administration: Oral
Result: Reducing the level of AR protein in mice after 24 hours.
Animal Model: SCID mice[1]
Dosage: 10, 20, and 40 mg/kg
Administration: P.o.; daily for 21 days
Result: Inhibits tumor growth by 46, 69, and 63%, respectively.
Animal Model: Male ICR Mice[1]
Dosage: 5 mg/kg
Administration: P.o. (Pharmacokinetic Analysis)
Result: The Cmax, AUC0-t and t1/2 were 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively.
Molecular Weight

820.37

Formula

C45H50ClN7O6
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C(N[C@H]1C(C)(C)[C@H](OC2=CC=C(C#N)C(Cl)=C2)C1(C)C)C3=CC=C(N4CCN(CC5CCN(C6=CC7=C(C(N(C(CC8)C(NC8=O)=O)C7=O)=O)C=C6)CC5)CC4)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (121.90 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 1.2190 mL 6.0948 mL 12.1896 mL
5 mM 0.2438 mL 1.2190 mL 2.4379 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 (sealed storage, away from moisture and light). 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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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

Purity: 99.40%

COA (244 KB) HNMR (465 KB) LCMS (92 KB)

Handling Instructions (2659 KB)
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 (sealed storage, away from moisture and light). 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 1.2190 mL 6.0948 mL 12.1896 mL 30.4741 mL
5 mM 0.2438 mL 1.2190 mL 2.4379 mL 6.0948 mL
10 mM 0.1219 mL 0.6095 mL 1.2190 mL 3.0474 mL
15 mM 0.0813 mL 0.4063 mL 0.8126 mL 2.0316 mL
20 mM 0.0609 mL 0.3047 mL 0.6095 mL 1.5237 mL
25 mM 0.0488 mL 0.2438 mL 0.4876 mL 1.2190 mL
30 mM 0.0406 mL 0.2032 mL 0.4063 mL 1.0158 mL
40 mM 0.0305 mL 0.1524 mL 0.3047 mL 0.7619 mL
50 mM 0.0244 mL 0.1219 mL 0.2438 mL 0.6095 mL
60 mM 0.0203 mL 0.1016 mL 0.2032 mL 0.5079 mL
80 mM 0.0152 mL 0.0762 mL 0.1524 mL 0.3809 mL
100 mM 0.0122 mL 0.0609 mL 0.1219 mL 0.3047 mL
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ARD-2128 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:

ARD-21282222111-87-5ARD2128ARD 2128PROTACsAndrogen ReceptorAR-regulatedtumorprostatecancerorallybioavailableInhibitorinhibitorinhibit

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