Description
Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay.
Product information
CAS Number: 1297538-32-9
Molecular Weight: 398.85
Formula: C19H19ClN6O2
Chemical Name: N-[(2S)-1-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]propan-2-yl]-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide
Smiles: C[C@@H](CN1C=CC(=N1)C1C=CC(C#N)=C(Cl)C=1)NC(=O)C1C=C(NN=1)C(C)O
InChiKey: BLIJXOOIHRSQRB-PXYINDEMSA-N
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
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 125 mg/mL (313.40 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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 enzalutamide or ARN-509, IC50 values being 230 and 170 nM for Darolutamide and ORM-15341 vs. 410 and 420 nM for enzalutamide and 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) 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 Darolutamide twice daily do not decrease significantly during the treatment.
Products are for research use only. Not for human use.
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