| Identification | Back Directory | [Name]
N-[4-Cyano-3-(trifluoromethyl)phenyl]-N′-[2-(2-thienyl)ethenyl]urea | [CAS]
1898232-70-6 | [Synonyms]
N-[4-Cyano-3-(trifluoromethyl)phenyl]-N′-[2-(2-thienyl)ethenyl]urea | [Molecular Formula]
C15H10F3N3OS | [MOL File]
1898232-70-6.mol | [Molecular Weight]
337.32 |
| Chemical Properties | Back Directory | [Boiling point ]
457.3±45.0 °C(Predicted) | [density ]
1.42±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted) | [form ]
Solid | [pka]
12.25±0.46(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1[1]. | [in vivo]
SC428 (60 mg/kg; intraperitoneal injection; once daily; 18 days) inhibited AR-V7 tumor growth by inducing tumor cell apoptosis in mice[1].
SC428 (90 mg/kg; intraperitoneal injection; five times a week; 3 weeks) inhibited the growth of AR-V7 in mice[1]. | Animal Model: | 22Rv1 cells were subcutaneously injected into the right flank of male Nu/Nu mice[1]. | | Dosage: | 60 mg/kg | | Administration: | Intraperitoneal injection (i.p.) ; daily route 5 days a week; 3 weeks | | Result: | Reduced the tumor growth by 50% , the mice did not lose weight, and the tumor PSA was reduced to undetectable levels. |
| Animal Model: | 22Rv1 cells were subcutaneously injected into the right flank of male Nu/Nu mice. Male Nu/Nu mice were surgically castrated when the implanted 22Rv1 cells achieved an average tumor size of 200 mm3[1]. | | Dosage: | 90 mg/kg | | Administration: | Intraperitoneal injection (i.p.); daily route 5 days a week; 3 weeks | | Result: | Inhibited the growth of prostate cancer with high expression of AR-V7.Good drug tolerance, no significant weight loss. |
| [References]
[1] Qianhui Yi , et al. Discovery of a Small-Molecule Inhibitor Targeting the Androgen Receptor N-Terminal Domain for Castration-Resistant Prostate Cancer. 2023 May 4;22(5):570-582. DOI:10.1158/1535-7163.MCT-22-0237 |
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