ODM-201

A potent wt/mutant androgen receptor (AR) inhibitor with Ki of 11 nM; inhibits wtAR/AR (F876L) with IC50 of 65/66 nM respectively, weak inhibition on AR (W741L) and AR (T877A) ; inhibits the nuclear translocation of AR and more efficaciously than enzalutamide or ARN-509 in VCaP cell line proliferation assay; reduces the growth of AR-overexpressing VCaP prostate cancer cells both in vitro and in a castration-resistant VCaP xenograft model.Prostate Cancer Phase 3 Clinical (In Vitro) :In competitive AR binding assays, the inhibition constant (Ki) values of Darolutamide (ODM-201) are 11 nM. ODM-201and ORM-15341 suppresse androgen-induced cell proliferation more efficaciously than ARN-509, IC50 values being 230 and 170 nM for Darolutamide and ORM-15341 vs. 420 nM for ARN-509. Darolutamide 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 Darolutamide and ORM-15341 are specific to AR-dependent PC cells. (In Vivo) :Darolutamide (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), 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 Darolutamide twice daily do not decrease significantly during the treatment.

1297538-32-9

BAY-1841788 | Darolutamide

>98% (HPLC)

DMSO: ≥ 44 mg/mL

O=C (C1=NNC (C (O) C) =C1) N[C@@H] (C) CN2N=C (C3=CC=C (C#N) C (Cl) =C3) C=C2

C19H19ClN6O2

398.8462

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.