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| Cas No.: | 1297538-32-9 |
| Chemical Name: | BAY-1841788,ODM-021,0DM021,ODM 021 |
| Synonyms: | BAY-1841788,ODM-021,0DM021,ODM 021 |
| SMILES: | N1N=C(C(=O)N[C@H](CN2N=C(C3C=C(Cl)C(C#N)=CC=3)C=C2)C)C=C1C(C)O |
| Formula: | C19H19ClN6O2 |
| M.Wt: | 398.85 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | ODM-201 is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in AR-HEK293 cells. |
| In Vivo: | ODM-201 showes a significant antitumor activity with both doses, 50 mg/kg twice daily being more efficacious compared to castrated, untreated mice (p < 0.001) or enzalutamide (p = 0.0245), which also showes inhibition of tumor growth (p < 0.05) vs. castrated, untreated mice. Further, there is no sign of treatment-related toxicities; the body weights of mice treated with ODM-201 twice daily do not decrease significantly during the treatment[1]. |
| In Vitro: | In competitive AR binding assays, the inhibition constant (Ki) values of ODM-201 are 11 nM. ODM-201and ORM-15341 suppresse androgen-induced cell proliferation more efficaciously than enzalutamide or ARN-509, IC50 values being 230 and 170 nM for ODM-201 and ORM-15341 vs. 410 and 420 nM for enzalutamide and ARN-509. ODM-201 has no effect on the viability of AR-negative cell lines tested, DU-145 prostate cancer cells and H1581 lung cancer cells confirming that the antiproliferative properties of ODM-201 and ORM-15341 are specific to AR-dependent PC cells[1]. |