
ODM-201
CAS No. 1297538-32-9
ODM-201( BAY-1841788 | Darolutamide )
Catalog No. M11201 CAS No. 1297538-32-9
A potent wt/mutant androgen receptor (AR) inhibitor with Ki of 11 nM.
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
2MG | 58 | In Stock |
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5MG | 96 | In Stock |
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10MG | 152 | In Stock |
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25MG | 251 | In Stock |
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50MG | 357 | In Stock |
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100MG | 531 | In Stock |
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500MG | 1152 | In Stock |
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1G | Get Quote | In Stock |
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Biological Information
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Product NameODM-201
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NoteResearch use only, not for human use.
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Brief DescriptionA potent wt/mutant androgen receptor (AR) inhibitor with Ki of 11 nM.
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DescriptionA 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.
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In Vitro——
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In Vivo——
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SynonymsBAY-1841788 | Darolutamide
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PathwayEndocrinology/Hormones
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TargetAndrogen Receptor (AR)
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RecptorAndrogenReceptor
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Research AreaCancer
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IndicationProstate Cancer
Chemical Information
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CAS Number1297538-32-9
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Formula Weight398.8462
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Molecular FormulaC19H19ClN6O2
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 44 mg/mL
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SMILESO=C(C1=NNC(C(O)C)=C1)N[C@@H](C)CN2N=C(C3=CC=C(C#N)C(Cl)=C3)C=C2
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Chemical Name1H-Pyrazole-3-carboxamide, N-[(1S)-2-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Moilanen AM, et al. Sci Rep. 2015 Jul 3;5:12007.
2. Fizazi K, et al. Lancet Oncol. 2014 Aug;15(9):975-85.
3. Cancer Discov. 2014 Sep;4(9):OF10.
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