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Proxalutamide

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Category SARS-CoV
CAS 1398046-21-3
Description Proxalutamide is a non-steroidal androgen receptor (AR) antagonist with potential anti-tumor activity for the treatment of prostate cancer and breast cancer.
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Product Information

Synonyms GT 0918; pruxelutamide; Benzonitrile, 4-[4,4-dimethyl-3-[6-[3-(2-oxazolyl)propyl]-3-pyridinyl]-5-oxo-2-thioxo-1-imidazolidinyl]-3-fluoro-2-(trifluoromethyl)-
IUPAC 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
Molecular Weight 517.5
Molecular Formula C24H19F4N5O2S
Canonical SMILES CC1(C(=O)N(C(=S)N1C2=CN=C(C=C2)CCCC3=NC=CO3)C4=C(C(=C(C=C4)C#N)C(F)(F)F)F)C
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
InChIKey KCBJGVDOSBKVKP-UHFFFAOYSA-N
Boiling Point 615.9±65.0 °C at 760 mmHg
Purity 98.79%
Density 1.48±0.1 g/cm3(Predicted)
Solubility Soluble in DMSO
Appearance Solid Powder
Storage Store at -20°C
Complexity 894
Exact Mass 517.11955869
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%.
Target Androgen Receptor; SARS-CoV
XLogP3-AA 4.3

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