For research use only. Not for therapeutic Use.
ODM-201(Cat No.: I001142) is a potent and full antagonist for the human androgen receptor (hAR). It belongs to the class of antiandrogen drugs and is primarily used in the treatment of prostate cancer. ODM-201 works by blocking the binding of androgens (male sex hormones) to the androgen receptor, thereby inhibiting the growth and proliferation of prostate cancer cells. It has demonstrated efficacy in clinical trials and is being investigated as a potential treatment option for patients with metastatic castration-resistant prostate cancer. ODM-201 offers an alternative to other antiandrogen drugs and may provide improved therapeutic outcomes for individuals with prostate cancer.
| Catalog Number | I001142 |
| CAS Number | 1297538-32-9 |
| Molecular Formula | C₁₉H₁₉ClN₆O₂ |
| Purity | 98% |
| Target | Androgen receptor |
| Target Protein | |
| Solubility | DMSO: ≥ 44 mg/mL |
| Appearance | Solid |
| Storage | Dry, dark and at 2 - 8 °C for six months or -20°C for two years. |
| IC50 | IC50: 26 nM (AR-HEK293 cells, AR) |
| IUPAC Name | N-[(2S)-1-[3-(3-chloro-4-cyanophenyl)pyrazol-1-yl]propan-2-yl]-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide |
| InChI | InChI=1S/C19H19ClN6O2/c1-11(22-19(28)18-8-17(12(2)27)23-24-18)10-26-6-5-16(25-26)13-3-4-14(9-21)15(20)7-13/h3-8,11-12,27H,10H2,1-2H3,(H,22,28)(H,23,24)/t11-,12?/m0/s1 |
| InChIKey | BLIJXOOIHRSQRB-PXYINDEMSA-N |
| SMILES | C[C@@H](CN1C=CC(=N1)C2=CC(=C(C=C2)C#N)Cl)NC(=O)C3=NNC(=C3)C(C)O |
| Reference | </br>1:Darolutamide (ODM-201) for the treatment of prostate cancer. Shore ND.Expert Opin Pharmacother. 2017 May 11. doi: 10.1080/14656566.2017.1329820. [Epub ahead of print] PMID: 28490267 </br>2:ODM-201 tablets complete phase I. Fenner A.Nat Rev Urol. 2015 Dec;12(12):654. doi: 10.1038/nrurol.2015.268. Epub 2015 Nov 3. No abstract available. PMID: 26526759 </br>3:Pharmacokinetics, Antitumor Activity, and Safety of ODM-201 in Patients with Chemotherapy-naive Metastatic Castration-resistant Prostate Cancer: An Open-label Phase 1 Study. Massard C, Penttinen HM, Vjaters E, Bono P, Lietuvietis V, Tammela TL, Vuorela A, Nykänen P, Pohjanjousi P, Snapir A, Fizazi K.Eur Urol. 2016 May;69(5):834-40. doi: 10.1016/j.eururo.2015.09.046. Epub 2015 Oct 17. PMID: 26463318 Free Article</br>4:ODM-201: a new-generation androgen receptor inhibitor in castration-resistant prostate cancer. Fizazi K, Albiges L, Loriot Y, Massard C.Expert Rev Anticancer Ther. 2015;15(9):1007-17. doi: 10.1586/14737140.2015.1081566. Review. PMID: 26313416 Free PMC Article</br>5:Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies. Moilanen AM, Riikonen R, Oksala R, Ravanti L, Aho E, Wohlfahrt G, Nykänen PS, Törmäkangas OP, Palvimo JJ, Kallio PJ.Sci Rep. 2015 Jul 3;5:12007. doi: 10.1038/srep12007. PMID: 26137992 Free PMC Article</br>6:Re: activity and safety of ODM-201 in patients with progressive metastatic castration-resistant prostate cancer (ARADES): an open-label phase 1 dose-escalation and randomised phase 2 dose expansion trial. Bjartell A.Eur Urol. 2015 Feb;67(2):348-9. doi: 10.1016/j.eururo.2014.11.019. No abstract available. PMID: 25760250 </br>7:ODM-201 is safe and active in metastatic castration-resistant prostate cancer. [No authors listed]Cancer Discov. 2014 Sep;4(9):OF10. doi: 10.1158/2159-8290.CD-RW2014-150. Epub 2014 Jul 9. PMID: 25185192 Free Article</br>8:Activity and safety of ODM-201 in patients with progressive metastatic castration-resistant prostate cancer (ARADES): an open-label phase 1 dose-escalation and randomised phase 2 dose expansion trial. Fizazi K, Massard C, Bono P, Jones R, Kataja V, James N, Garcia JA, Protheroe A, Tammela TL, Elliott T, Mattila L, Aspegren J, Vuorela A, Langmuir P, Mustonen M; ARADES study group..Lancet Oncol. 2014 Aug;15(9):975-85. doi: 10.1016/S1470-2045(14)70240-2. Epub 2014 Jun 25. PMID: 24974051 |
