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Art. -Nr.: HY-162702

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AZ'3137

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AZ‘3137 is an orally active PROTAC-type androgen receptor (AR) degrader with a DC₅₀ value of 22 nM. AZ‘3137 can degrade L702H mutant AR (DC₅₀ of 92 nM). AZ'3137 can inhibit cell proliferation of LNCaP, with a GI₅₀ value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice.
(Pink: Androgen Receptor ligand (HY-172954); Blue: Cereblon ligand (HY-172955); Black: linker (HY-W262798)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.90%
CAS. Nr.: 2960179-55-7
Formel: C₄₃H₄₇F₄N₇O₄
Molecular Weight:801.87

Speicherung:

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

AZ'3137 Chemical Structure

CAS. Nr.: 2960179-55-7

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Amount: USD 0.00

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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

Biologische Aktivität

Beschreibung

AZ‘3137 is an orally active PROTAC-type androgen receptor (AR) degrader with a DC₅₀ value of 22 nM. AZ‘3137 can degrade L702H mutant AR (DC₅₀ of 92 nM). AZ'3137 can inhibit cell proliferation of LNCaP, with a GI₅₀ value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice^[1]. (Pink: Androgen Receptor ligand (HY-172954); Blue: Cereblon ligand (HY-172955); Black: linker (HY-W262798)).

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
LNCaP	GI₅₀	74 nM Compound: 22; AZ'3137	Anti-proliferative activity against human LNCaP cells assessed as number of live cells measured after 7 days by Sytox Green Nucleic Acid stain assay Anti-proliferative activity against human LNCaP cells assessed as number of live cells measured after 7 days by Sytox Green Nucleic Acid stain assay	[PMID: 38991141]

In Vitro

AZ'3137 (Compound 22; 0-10 μM; 7 days) can inhibit AR signaling and cell proliferation of prostate cancer cell line LNCaP^[1].
AZ′3137 (0.1 nM-10 μM; 24 h) inhibits the expression of AR target genes in LNCaP cells^[1].
AZ′3137 (0.1 nM-10 μM; 24 h) is able to degrade AR in C4-2 and VCAP cells^[1].

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

Cell Proliferation Assay^[1].

Cell Line:

LNCaP cells
Concentration:

0-10 μM
Incubation Time:

7 days
Result:

Inhibited the proliferation of LNCaPs with a GI₅₀ value of 74 nM.

RT-PCR^[1].

Cell Line:

LNCaP cells
Concentration:

0.1 nM, 1 nM, 10 nM, 100 nM, 1 μM, 10 μM
Incubation Time:

24 h
Result:

Was able to inhibit the expression of AR target genes.

Western Blot Analysis^[1].

Cell Line:

C42 cells and VCAP cells
Concentration:

0.1 nM, 0.3 nM, 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 μM, 3 μM, 10 μM
Incubation Time:

24 h
Result:

Was able to degrade AR.

In Vivo

AZ'3137 (Compound 22; oral gavage (p.o.); once daily; for 10 days) inhibits tumor growth in prostate cancer mice^[1].

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

Animal Model:

Immunocompromised NOD SCID male mice implanted with C4-2 cell subcutaneous tumors^[1].
Dosage:

30 mg/kg
Administration:

Oral gavage (p.o.); once daily; for 10 days
Result:

Degraded AR and inhibited tumor growth.

Chemical Information

CAS. Nr. 2960179-55-7
Appearance Solid
Molecular Weight 801.87
Formel C₄₃H₄₇F₄N₇O₄
Color White to off-white
SMILES

COC1=CC(N2CCN(CC3CCN(C4=CC=C(C5CCN(C6=CC=C(C#N)C(C(F)(F)F)=C6F)CC5)C=C4)CC3)CC2)=CC7=C1C(N(C8CCC(NC8=O)=O)C7)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (62.35 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

1.2471 mL

6.2354 mL

12.4708 mL

5 mM

0.2494 mL

1.2471 mL

2.4942 mL

10 mM

0.1247 mL

0.6235 mL

1.2471 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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Bagal SK, et al. Discovery of a Series of Orally Bioavailable Androgen Receptor Degraders for the Treatment of Prostate Cancer. J Med Chem. 2024 Jul 25;67(14):11732-11750. [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	1.2471 mL	6.2354 mL	12.4708 mL	31.1771 mL
	5 mM	0.2494 mL	1.2471 mL	2.4942 mL	6.2354 mL
	10 mM	0.1247 mL	0.6235 mL	1.2471 mL	3.1177 mL
	15 mM	0.0831 mL	0.4157 mL	0.8314 mL	2.0785 mL
	20 mM	0.0624 mL	0.3118 mL	0.6235 mL	1.5589 mL
	25 mM	0.0499 mL	0.2494 mL	0.4988 mL	1.2471 mL
	30 mM	0.0416 mL	0.2078 mL	0.4157 mL	1.0392 mL
	40 mM	0.0312 mL	0.1559 mL	0.3118 mL	0.7794 mL
	50 mM	0.0249 mL	0.1247 mL	0.2494 mL	0.6235 mL
	60 mM	0.0208 mL	0.1039 mL	0.2078 mL	0.5196 mL

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MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

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AZ'3137

Anti-Cancer Compound Library

Orally Active Compound Library

Transcription Factor-Targeted Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

PROTAC Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZ'3137

Anti-Cancer Compound Library

Orally Active Compound Library

Transcription Factor-Targeted Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

PROTAC Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZ'3137 Related Classifications

HY-162702 Related Classifications