Cat. No.: HY-152850

Gumelutamide

Name: Gumelutamide
Brand: MedChemExpress
SKU: HY-152850
Price: 300.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: TAS3681)

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Based on 1 Customer Validation

Gumelutamide (TAS3681) is an orally active androgen receptor (AR) antagonist with an IC₅₀ of 52.7 nM in COS-7 cells. Gumelutamide binds to AR, blocks nuclear translocation and DNA binding, and antagonizes full-length AR, AR mutants, and AR splice variants. Gumelutamide induces apoptosis and inhibits androgen-dependent proliferation in AR-positive prostate cancer cells. Gumelutamide can be used in research on metastatic castration-resistant prostate cancer and prostate cancer.

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

Purity : 99.00%
CAS No.: 1831085-48-3
Formula: C₂₂H₂₁ClN₆O
Molecular Weight:420.89

Storage:

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

Gumelutamide Chemical Structure

CAS No.: 1831085-48-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]^[2]^[3]

AR-V7

AR-FL

AR-Vs

In Vitro

Anti-cancerApoptosisCell Cycle RegulationOthers

Anti-cancer

Gumelutamide (TAS3681) (3-1000 nM; 1 day) antagonizes wild-type AR transactivation in VCaP cells with an IC₅₀ of 60.9 nM^[3].
Gumelutamide (3-1000 nM; 1 day) antagonizes T878A mutant AR transactivation in LNCaP cells with an IC₅₀ of 10.1 nM^[3].
Gumelutamide (1-10000 nM; 3 days) inhibits DHT-induced VCaP cell viability with an IC₅₀ of 170 nM^[3].
Gumelutamide (1-10000 nM; 3 days) inhibits DHT-induced LNCaP cell viability with an IC₅₀ of 18 nM^[3].
Gumelutamide (6 days) inhibits DHT-induced proliferation of parental LNCaP cells and F877L-expressing LNCaP cells^[3].
Gumelutamide (1-10 μM; 1 day) downregulates AR protein in LNCaP cells, reducing relative AR expression to 0.2 at 7 and 10 μM^[3].
Gumelutamide (1-10 μM; 1 day) downregulates AR protein in VCaP cells^[3].
Gumelutamide (1 μM; 4.5 h) blocks DHT-induced AR nuclear translocation in U-2 OS tomato-AR cells with an IC₅₀ of 63.7 nM, and does not induce AR nuclear translocation in the absence of DHT^[3].
Gumelutamide (1-10 μM; 1 day) downregulates AR-FL and AR-Vs proteins in SAS MDV No. 3-14 cells^[3].
Gumelutamide (1-10 μM; 1 day) downregulates nuclear and cytoplasmic AR-FL and AR-Vs in SAS MDV No. 3-14 cells^[3].
Gumelutamide downregulates AR-FL and AR-V7 proteins in 22Rv1 cells^[3].
Gumelutamide (3-10 μM; 3-9 days) inhibits the proliferation of Enzalutamide (HY-70002)-resistant SAS MDV No. 3-14 cells^[3].

Anti-cancer

Apoptosis

Gumelutamide (1-10 μM; 1 day) induces cPARP-associated apoptosis in SAS MDV No. 3-14 cells^[3].

Anti-cancer

Cell Cycle Regulation

Gumelutamide (7.5 μM; 1 day) reduces the expression of AR-V7 target genes, including UBE2C^[3], in SAS MDV No. 3-14 cells.

Others

Gumelutamide (20 h) binds to wild-type AR in cell lysates with a K_i of 7.39 nM and to T878A mutant AR with a K_i of 23.8 nM^[3].
Gumelutamide (3-1000 nM; 1 day) antagonizes wild-type AR transactivation in COS-7 cells with an IC₅₀ of 52.7 nM^[3].

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

Cell Viability Assay^[3]

Cell Line:

VCaP cells
Concentration:

1, 10, 100, 10000 nM
Incubation Time:

3 days
Result:

Dose-dependently suppressed DHT-induced VCaP cells viability with IC₅₀ 170 nM.

Cell Viability Assay^[3]

Cell Line:

LNCaP cells
Concentration:

1, 10, 100, 10000 nM
Incubation Time:

3 days
Result:

Dose-dependently suppressed LNCaP cells viability with IC₅₀ 18 nM.

Western Blot Analysis^[3]

Cell Line:

LNCaP cells
Concentration:

1, 3, 5, 7, 10 μM
Incubation Time:

1 day
Result:

Reduced AR protein dose-dependently, with relative AR expression values of 0.6, 0.4, 0.4, 0.2, and 0.2 at 1, 3, 5, 7, and 10 μM, respectively, versus DMSO set at 1.0.

Immunofluorescence^[3]

Cell Line:

U-2 OS tomato-AR cells
Concentration:

1 μM
Incubation Time:

0.5 h preincubation; 4 h incubation
Result:

Dose-dependently blocked DHT-induced AR nuclear translocation with IC₅₀ 63.7 nM.

Western Blot Analysis^[3]

Cell Line:

SAS MDV No. 3-14 cells
Concentration:

1, 3, 5, 7, 10 μM
Incubation Time:

1 day
Result:

Dose-dependently reduced both AR-FL and AR-Vs protein levels.\nReduced both AR-FL and AR-Vs expression in cytoplasmic and nuclear fractions.\nInduced cPARP expression in SAS MDV No. 3-14 cells.

Real Time qPCR^[3]

Cell Line:

SAS MDV No. 3-14 cells
Concentration:

7.5 μM
Incubation Time:

1 day
Result:

Decreased expression of AR-V7 target genes including UBE2C in both the absence and presence of DHT.

In Vivo

Anti-cancer

Gumelutamide (TAS3681) (7.5-22.5 mg/kg; oral gavage; twice daily; 14 days) suppresses tumor growth and reduces serum PSA and tumor AR-FL/AR-Vs levels in castrated male SCID mice bearing an enzalutamide-resistant prostate cancer xenograft^[3].

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

Animal Model:

CB-17/Icr-scid/scidJcl (SCID; male; 5 weeks old at purchase; castrated at 6 weeks of age)^[3]
Dosage:

7.5 mg/kg; 15 mg/kg; 22.5 mg/kg
Administration:

oral gavage; twice daily; 14 days
Result:

Mean relative tumor volume ratios to vehicle control (T/C ratio) were 64%, 41%, and 24% at 7.5, 15, and 22.5 mg/kg, respectively.
Tumor regression was observed in 1 of 10 mice at 15 mg/kg and 3 of 10 mice at 22.5 mg/kg.
Serum PSA levels decreased dose-dependently.
AR-FL and AR-Vs protein expression in harvested tumors was dose-dependently downregulated.

Related Protocols :

Chemical Information

CAS No. 1831085-48-3
Appearance Solid
Molecular Weight 420.89
Formula C₂₂H₂₁ClN₆O
Color Off-white to light yellow
SMILES

N#CC1=CC=C(N2CC3=C(CC2)C(NC4=NC=C(C(C)(C)O)C=C4)=NC=N3)C=C1Cl
Synonyms

TAS3681
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 : 50 mg/mL (118.80 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

2.3759 mL

11.8796 mL

23.7592 mL

5 mM

0.4752 mL

2.3759 mL

4.7518 mL

10 mM

0.2376 mL

1.1880 mL

2.3759 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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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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.

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (299 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)

References

[1]. Bernard-Tessier A, et al. The future of androgen receptor targeting in prostate cancer: third-generation inhibitors and beyond. Ther Adv Med Oncol. 2025 Sep 29;17:17588359251379416.

[2]. World Health Organization. International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 128. WHO Drug Information. 2022;36(4).

[3]. Yoshida S, et al. TAS3681, an androgen receptor antagonist, prevents drug resistance driven by aberrant androgen receptor signaling in prostate cancer. Molecular oncology. 2024 Aug;18(8):1980-2000. [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	2.3759 mL	11.8796 mL	23.7592 mL	59.3979 mL
	5 mM	0.4752 mL	2.3759 mL	4.7518 mL	11.8796 mL
	10 mM	0.2376 mL	1.1880 mL	2.3759 mL	5.9398 mL
	15 mM	0.1584 mL	0.7920 mL	1.5839 mL	3.9599 mL
	20 mM	0.1188 mL	0.5940 mL	1.1880 mL	2.9699 mL
	25 mM	0.0950 mL	0.4752 mL	0.9504 mL	2.3759 mL
	30 mM	0.0792 mL	0.3960 mL	0.7920 mL	1.9799 mL
	40 mM	0.0594 mL	0.2970 mL	0.5940 mL	1.4849 mL
	50 mM	0.0475 mL	0.2376 mL	0.4752 mL	1.1880 mL
	60 mM	0.0396 mL	0.1980 mL	0.3960 mL	0.9900 mL
	80 mM	0.0297 mL	0.1485 mL	0.2970 mL	0.7425 mL
	100 mM	0.0238 mL	0.1188 mL	0.2376 mL	0.5940 mL

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Gumelutamide