Art. -Nr.: HY-164807

SARD279

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SARD279 is a HyT degrader of androgen receptor (AR). SARD279 binds to AR, recruits HSP70, mediates ubiquitin-dependent proteasomal degradation, and competitively inhibits the transactivation of AR. SARD279 exhibits antiproliferative activity in AR-dependent prostate cancer cells and castration-resistant prostate cancer cells, including those harboring the AR^F876L mutation. SARD279 can be used in studies related to prostate cancer and castration-resistant prostate cancer.
(Pink: Androgen Receptor ligand (HY-117486); Blue: HyT ligand (HY-W001578); Black: linker (HY-W004896)).

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Reinheit: 96.04%
CAS. Nr.: 1489236-55-6
Formel: C₃₃H₄₁F₃N₄O₅S
Molecular Weight:662.76

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

SARD279 Chemical Structure

CAS. Nr.: 1489236-55-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

SARD279 is a HyT degrader of androgen receptor (AR). SARD279 binds to AR, recruits HSP70, mediates ubiquitin-dependent proteasomal degradation, and competitively inhibits the transactivation of AR. SARD279 exhibits antiproliferative activity in AR-dependent prostate cancer cells and castration-resistant prostate cancer cells, including those harboring the AR^F876L mutation. SARD279 can be used in studies related to prostate cancer and castration-resistant prostate cancer^[1]^[2]^[3]^[4]^[5]. (Pink: Androgen Receptor ligand (HY-117486); Blue: HyT ligand (HY-W001578); Black: linker (HY-W004896)).

IC₅₀ & Target^[1]^[2]^[3]^[4]^[5]

HSP70

Alle HSP Isoform-spezifische Produkte anzeigen :

In Vitro

SARD279 (0-10000 nM; 20 h) degrades androgen receptor in VCaP prostate cancer cells with a DC₅₀ of 1099 nM and a maximum degradation of 69% after 20 hours of treatment^[1].
SARD279 (156 nM-10 μM) induces HSP70-dependent, selective degradation of androgen receptor (AR) in LNCaP human prostate cancer cells, inhibits AR-dependent gene expression with an IC₅₀ of 156 nM, and exerts antiproliferative effects in AR-dependent and castration-resistant prostate cancer cell lines^[2].
SARD279 (10 μM; 24 h) mediates Hsp70-associated degradation of androgen receptor in LNCaP human prostate tumor cells with a DC₅₀ of 1 μM and achieves complete AR degradation at 10 μM^[3].
SARD279 (500 nM-10 μM; 24 h) induces proteasome-dependent degradation of the androgen receptor in LNCaP human prostate tumor cells with a DC₅₀ of 1 μM, and this activity is enhanced by Hsp90 inhibition^[5].
SARD279 antagonizes androgen receptor target gene expression in AR-overexpressing LNCaP-AR human prostate tumor cells without exhibiting agonist activity^[5].
SARD279 (3 μM; 9 days) specifically suppresses proliferation of AR-dependent LNCaP human prostate tumor cells, with no effect on AR-independent cell lines^[5].
SARD279 (0.01-10 μM; 7 days) retains dose-dependent antiproliferative activity in LNCaP human prostate tumor cells in the presence of 1 nM R1881, overcoming androgen-mediated resistance to MDV3100^[5].
SARD279 (0.01-3 μM; 7 days) exerts dose-dependent antiproliferative effects in MDV3100-resistant LNCaP/AR^F876L human prostate tumor cells, overcoming F876L mutation-mediated resistance^[5].
Pre-fused SARD279 (0.03-0.5 μM; 24 h) (with HSP70, delivered via 80-O14B LNPs) potently degrades androgen receptor in LNCaP cells with a DC₅₀ of ~0.06 μM, while free SARD279 (0.12-0.5 μM; 24 h) shows no AR degradation at concentrations up to 0.5 μM^[4].
SARD279 binds directly to the androgen receptor with reduced affinity (37-fold lower than RU59063)^[5].
SARD279 blocks androgen receptor transactivation in 293 cells with an IC₅₀ of 156 nM^[5].

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

Western Blot Analysis^[1]

Cell Line:

VCaP prostate cancer cells
Concentration:

0-10000 nM
Incubation Time:

20 h
Result:

Induced AR degradation in VCaP cells, achieving a maximum degradation (Dmax) of 69% and a half-maximal degradation concentration (DC₅₀) of 1099 nM.

Western Blot Analysis^[4]

Cell Line:

LNCaP cells
Concentration:

0.03-0.5 μM (pre-fused SARD279); 0.12-0.5 μM (free SARD279)
Incubation Time:

24 h (pre-fused SARD279); 24 h (free SARD279)
Result:

Showed no AR degradation in LNCaP cells at concentrations from 0.125 to 0.5 μM (free SARD279).
Achieved more than 80% AR degradation at 0.5 μM (pre-fused SARD279 with HSP70 delivered via LNPs).
Exhibited concentration-dependent degradation with a DC₅₀ of approximately 0.06 μM (pre-fused SARD279), which is about 16 times lower than the DC₅₀ of free SARD279.
Showed no increase in AR degradation efficiency when LNPs were added alone.

Western Blot Analysis^[5]

Cell Line:

LNCaP human prostate tumor cells
Concentration:

500 nM, 1 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time:

24 h
Result:

Reduced AR protein levels in a concentration-dependent manner, with a DC₅₀ of 1 μM.
Blocked SARD279-induced AR degradation by co-incubation with the competitive AR agonist RU59063.
Prevented SARD279-induced AR degradation by pretreatment/co-treatment with the proteasome-specific inhibitor epoxomicin.
Enhanced AR degradation at sub-DC₅₀ concentrations when co-incubated with the Hsp90 inhibitor geldanamycin (at concentrations that did not affect AR levels alone).

Cell Proliferation Assay^[5]

Cell Line:

LNCaP human prostate tumor cells; HEK293T cells; PC3 human prostate cancer cells
Concentration:

3 μM
Incubation Time:

9 days
Result:

Suppressed LNCaP cell proliferation with similar efficacy to MDV3100 within 2 days.
Did not affect proliferation of AR-independent HEK293T and PC3 human prostate cancer cell lines.

Cell Proliferation Assay^[5]

Cell Line:

LNCaP human prostate tumor cells
Concentration:

0.01 μM, 0.1 μM, 1 μM, 10 μM
Incubation Time:

7 days
Result:

Exhibited dose-dependent antiproliferative activity in LNCaP cells treated with 1 nM R1881.
Showed retained antiproliferative efficacy while MDV3100 lost antiproliferative efficacy under these conditions.

Cell Proliferation Assay^[5]

Cell Line:

LNCaP/AR-F876L (MDV3100-resistant, AR-F876L mutant) human prostate tumor cells
Concentration:

0.01 μM, 0.3 μM, 1 μM, 3 μM
Incubation Time:

7 days
Result:

Exhibited dose-dependent antiproliferative activity in LNCaP/AR-F876L cells.
Showed antiproliferative effects while MDV3100 induced proliferation in these cells.

Chemical Information

CAS. Nr. 1489236-55-6
Appearance Solid
Molecular Weight 662.76
Formel C₃₃H₄₁F₃N₄O₅S
Color White to off-white
SMILES

O=C(OCCOCCNC(CCCN(C1(C)C)C(N(C(C=C2)=CC(C(F)(F)F)=C2C#N)C1=O)=S)=O)CC3(C[C@H](C4)C5)C[C@H]5C[C@H]4C3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (150.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5088 mL

7.5442 mL

15.0884 mL

5 mM

0.3018 mL

1.5088 mL

3.0177 mL

10 mM

0.1509 mL

0.7544 mL

1.5088 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (7.54 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (7.54 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (7.54 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Salami J, et al. Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellular models of prostate cancer drug resistance. Communications biology. 2018;1:100. [Content Brief]

[2]. Collins I, et al. Chemical approaches to targeted protein degradation through modulation of the ubiquitin-proteasome pathway. The Biochemical journal. 2017 Mar 15;474(7):1127-1147. [Content Brief]

[3]. Xie S, et al. Small-Molecule Hydrophobic Tagging: A Promising Strategy of Druglike Technology for Targeted Protein Degradation. Journal of medicinal chemistry. 2023 Aug 24;66(16):10917-10933. [Content Brief]

[4]. Chen J, et al. Enhanced protein degradation by intracellular delivery of pre-fused PROTACs using lipid-like nanoparticles. Journal of controlled release : official journal of the Controlled Release Society. 2021 Feb 10;330:1244-1249. [Content Brief]

[5]. Gustafson JL, et al. Small-Molecule-Mediated Degradation of the Androgen Receptor through Hydrophobic Tagging. Angewandte Chemie (International ed. in English). 2015 Aug 10;54(33):9659-62. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	1.5088 mL	7.5442 mL	15.0884 mL	37.7210 mL
	5 mM	0.3018 mL	1.5088 mL	3.0177 mL	7.5442 mL
	10 mM	0.1509 mL	0.7544 mL	1.5088 mL	3.7721 mL
	15 mM	0.1006 mL	0.5029 mL	1.0059 mL	2.5147 mL
	20 mM	0.0754 mL	0.3772 mL	0.7544 mL	1.8861 mL
	25 mM	0.0604 mL	0.3018 mL	0.6035 mL	1.5088 mL
	30 mM	0.0503 mL	0.2515 mL	0.5029 mL	1.2574 mL
	40 mM	0.0377 mL	0.1886 mL	0.3772 mL	0.9430 mL
	50 mM	0.0302 mL	0.1509 mL	0.3018 mL	0.7544 mL
	60 mM	0.0251 mL	0.1257 mL	0.2515 mL	0.6287 mL
	80 mM	0.0189 mL	0.0943 mL	0.1886 mL	0.4715 mL
	100 mM	0.0151 mL	0.0754 mL	0.1509 mL	0.3772 mL

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SARD279

Alle HSP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SARD279 Related Classifications

HY-164807 Related Classifications