Ketodarolutamide
CAS No. : 1297537-33-7
(Synonyms: BAY 1896953; ORM-15341)
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| Cat. No. : | HY-19337 |
| M.Wt: | 396.83 |
| Formula: | C19H17ClN6O2 |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells[1]. Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs[1]. Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) [1][2]. Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer[1][2].
In Vitro:Ketodarolutamide (ORM-15341) (24 h) exhibits a Ki value of 8 nM for rat wild-type AR (wtAR) and an IC50 value of 38 nM for human AR (hAR) in AR-HEK293 cells and shows IC50 values of 51 nM, 1160 nM and 700 nM against mutant AR variants (F876L, W741L, T877A) in U2-OS cells[1].
Ketodarolutamide (0.3 μM; 4 h) inhibits testosterone-induced nuclear translocation of AR in HS-HEK293 cells and LNCaP cells[1].
Ketodarolutamide (10-10000 nM; 4 days) suppresses androgen-induced proliferation of VCaP cells more potently than Enzalutamide (HY-70002) and has no effect on the viability of AR-negative DU-145 prostate cancer cells and H1581 lung cancer cells, as determined by cell proliferation assay[1].
In Vivo:Ketodarolutamide (ORM-15341) (metabolized from oral administration of ODM-201 (HY-16985) ) (50 mg/kg; oral administration; once or twice a day; for 37 days) exhibits potent antitumor activity in castrated male BALB/c nude mice bearing subcutaneous VCaP xenografts[1].
Ketodarolutamide (metabolized from oral administration of ODM-201) (50 mg/kg; oral administration; twice a day; for 3 weeks) does not increase serum testosterone levels in intact nude mice bearing orthotopic VCaP tumors[1].
Ketodarolutamide (metabolized from oral administration of ODM-201) (25, 50, 100 mg/kg; oral administration; twice a day; for 7 days) shows negligible blood-brain barrier penetration with a brain/plasma ratio of 1.9-2.8% in mice[1].
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