Darolutamide
CAS No. : 1297538-32-9
(Synonyms: ODM-201; BAY-1841788)
| Size | Price | Stock |
|---|---|---|
| 5mg | $132 | In-stock |
| 10mg | $209 | In-stock |
| 25mg | $366 | In-stock |
| 50mg | $495 | In-stock |
| 100mg | $690 | In-stock |
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| Cat. No. : | HY-16985 |
| M.Wt: | 398.85 |
| Formula: | C19H19ClN6O2 |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist. Darolutamide has a Ki of 11 nM for rat wild-type AR (wtAR) and IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation[1]. Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation[1]. Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants[1]. Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer[1].
IC50 & Target:IC50: 26 nM (AR-HEK293 cells, AR)[1]
In Vitro:Darolutamide (ODM-201) (0.1 nM-100 μM; 0-4 ℃ overnight) competitively binds to wild-type androgen receptor (wtAR) in cytosolic lysates from rat ventral prostates, with an inhibition constant (Ki) of 11 nM[1].
Darolutamide (0.1 nM-100 μM; 24 h) inhibits human wild-type AR (hAR)-mediated transcriptional activation in AR-HEK293 cells, with an IC50 of 26 nM[1].
Darolutamide (0.1 nM-100 μM; 24 h) acts as a full antagonist against mutant ARs (AR(F876L), AR(W741L), AR(T877A)) in transiently transfected U2-OS cells, with IC50 values of 66 nM, 1500 nM, and 1782 nM respectively[1].
Darolutamide (0.3 μM; 4 h) inhibits testosterone-induced AR nuclear translocation in AR-overexpressing HS-HEK293 cells[1].
Darolutamide (3 μM; 4 h) inhibits testosterone-induced AR nuclear translocation in AR-overexpressing LN-AR-C cells[1].
Darolutamide (10 nM-10 μM; 4 days) suppresses androgen-induced cell proliferation in VCaP cells (AR-overexpressing prostate cancer cells). Darolutamide also shows negligible cytotoxicity against AR-negative cells (DU-145 prostate cancer cells, H1581 lung cancer cells)[1].
In Vivo:Darolutamide (ODM-201) (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].
Darolutamide (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].
Darolutamide (25, 50, 100 mg/kg; oral administration; twice a day; for 7 days) shows negligible blood-brain barrier penetration with its major active metabolite Ketodarolutamide (HY-19337) having a brain/plasma ratio of 1.9-2.8% in mice[1].
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