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Biochem/physiol Actions
Compound 27c (cpd 27c) is a potent and selective inducer of E3 ligase MDM2-mediated degradation of androgen receptor (AR) and the constitutively active splice variant AR-V7 (DC50 = 2.67 and 2.64 μM, respectively, post 24h treatment in 22RV1 cells). Cpd 27c selectively inhibits AR-dependent proliferation in prostate cancer cultures (IC50 = 0.9 μM/22RV1 and 1.4 μM/LNCaP, >50 μM/AR-neg DU-145) and exhibits antitumor efficacy in an enzalutamide-resistant 22RV1 xenograft model in mice in vivo (10 or 30 mg/kg vial daily i.v.) by suppressing AR signaling pathway transcriptional activity.
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | -10 to -25°C |
| SMILES string | N#CC1=CC=C(N2C(N(CCNC3=C4C=CC=NC4=C(C=C3)F)C(C)(C)C2=O)=O)C=C1C(F)(F)F |
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