2. Vitamin D Related/Nuclear Receptor PROTAC
  3. Androgen Receptor PROTACs
  4. ARD-69

ARD-69 (compound 34) is a potent PROTAC androgen receptor degrader. ARD-69 induces degradation of androgen receptor (AR) protein in AR-positive prostate cancer cell lines. ARD-69 suppresses AR-regulated gene expression. ARD-69 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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ARD-69 Chemical Structure

ARD-69 Chemical Structure

CAS No. : 2316837-10-0

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1 mg USD 750 In-stock
5 mg USD 1600 In-stock
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50 mg USD 8350 In-stock
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Based on 1 publication(s) in Google Scholar

ARD-69 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

ARD-69 (compound 34) is a potent PROTAC androgen receptor degrader. ARD-69 induces degradation of androgen receptor (AR) protein in AR-positive prostate cancer cell lines. ARD-69 suppresses AR-regulated gene expression[1]. ARD-69 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

Androgen receptor (AR)[1]
PROTAC[1]
Cellular Effect
Cell Line Type Value Description References
CWR22R IC50
183 nM
Compound: 34; ARD-69
Cytotoxicity against AR-positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 7 days in regular culture medium by WST-8 assay
Cytotoxicity against AR-positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 7 days in regular culture medium by WST-8 assay
[PMID: 30629437]
LNCaP IC50
0.25 nM
Compound: 34; ARD-69
Cytotoxicity against AR-positive human LNCaP cells assessed as inhibition of cell growth incubated for 7 days in presence of AR agonist, R1881 in charcoal stripped medium by WST-8 assay
Cytotoxicity against AR-positive human LNCaP cells assessed as inhibition of cell growth incubated for 7 days in presence of AR agonist, R1881 in charcoal stripped medium by WST-8 assay
[PMID: 30629437]
VCaP IC50
0.34 nM
Compound: 34; ARD-69
Cytotoxicity against AR-positive human VCaP cells assessed as inhibition of cell growth incubated for 7 days in presence of AR agonist, R1881 in charcoal stripped medium by WST-8 assay
Cytotoxicity against AR-positive human VCaP cells assessed as inhibition of cell growth incubated for 7 days in presence of AR agonist, R1881 in charcoal stripped medium by WST-8 assay
[PMID: 30629437]
Molecular Weight

1129.82

Formula

C62H74ClFN8O7S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC(O[C@H]2C(C)(C)[C@H](NC(C3=CC=C(C#CC4CCN(C5CCN(C(C[C@H](NC([C@H]6N(C([C@@H](NC(C7(CC7)F)=O)C(C)(C)C)=O)C[C@H](O)C6)=O)C8=CC=C(C9=C(C)N=CS9)C=C8)=O)CC5)CC4)C=C3)=O)C2(C)C)=CC=C1C#N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 200 mg/mL (177.02 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8851 mL 4.4255 mL 8.8510 mL
5 mM 0.1770 mL 0.8851 mL 1.7702 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 (protect from light, stored under nitrogen). 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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In Vivo Dissolution Calculator
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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 (protect from light, stored under nitrogen). 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 0.8851 mL 4.4255 mL 8.8510 mL 22.1274 mL
5 mM 0.1770 mL 0.8851 mL 1.7702 mL 4.4255 mL
10 mM 0.0885 mL 0.4425 mL 0.8851 mL 2.2127 mL
15 mM 0.0590 mL 0.2950 mL 0.5901 mL 1.4752 mL
20 mM 0.0443 mL 0.2213 mL 0.4425 mL 1.1064 mL
25 mM 0.0354 mL 0.1770 mL 0.3540 mL 0.8851 mL
30 mM 0.0295 mL 0.1475 mL 0.2950 mL 0.7376 mL
40 mM 0.0221 mL 0.1106 mL 0.2213 mL 0.5532 mL
50 mM 0.0177 mL 0.0885 mL 0.1770 mL 0.4425 mL
60 mM 0.0148 mL 0.0738 mL 0.1475 mL 0.3688 mL
80 mM 0.0111 mL 0.0553 mL 0.1106 mL 0.2766 mL
100 mM 0.0089 mL 0.0443 mL 0.0885 mL 0.2213 mL
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ARD-69 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-692316837-10-0ARD69ARD 69Androgen ReceptorPROTACsAR-positive prostate cancer cell linesgene expressionInhibitorinhibitorinhibit

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