Proxalutamide (GT0918) is an orally active potent androgen receptor (AR) antagonist. Proxalutamide (GT0918) can be used in the study for prostate cancer.

Product information

CAS Number: 1398046-21-3

Molecular Weight: 517.50

Formula: C24H19F4N5O2S

Chemical Name: 4-(4,4-dimethyl-3-{6-[3-(1,3-oxazol-2-yl)propyl]pyridin-3-yl}-5-oxo-2-sulfanylideneimidazolidin-1-yl)-3-fluoro-2-(trifluoromethyl)benzonitrile

Smiles: CC1(C)C(=O)N(C(=S)N1C1=CC=C(CCCC2=NC=CO2)N=C1)C1=CC=C(C#N)C(=C1F)C(F)(F)F

InChiKey: KCBJGVDOSBKVKP-UHFFFAOYSA-N

InChi: InChI=1S/C24H19F4N5O2S/c1-23(2)21(34)32(17-9-6-14(12-29)19(20(17)25)24(26,27)28)22(36)33(23)16-8-7-15(31-13-16)4-3-5-18-30-10-11-35-18/h6-11,13H,3-5H2,1-2H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (193.24 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Proxalutamide (GT0918) down-regulates AR protein level in prostate cancer cells. Proxalutamide can overcome the resistance of prostatic cancer cells by downregulating the expression of AR genes. Proxalutamide (GT0918, 0-200 μM) dose-dependently inhibits cell viability in LNCaP and 22RV1.

In Vivo:

The elimination half-life (t1/2) of proxalutamide in rats is approximately 2 h regardless of whether it is administered by the intragastric or the intravenous route. The maximum plasma concentration of proxalutamide (Cmax) could reach 2 μg/mL or higher, and the oral absolute bioavailability (F) was approximately 80%.

Products are for research use only. Not for human use.