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Darolutamide

Cat. No. M9956
Darolutamide Structure
Synonym:

ODM-201; BAY-1841788

Size Price Availability Quantity
1mg USD 60  USD60 In stock
5mg USD 120  USD120 In stock
10mg USD 200  USD200 In stock
50mg USD 600  USD600 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Darolutamide (ODM-201) is a new-generation, potent and selective androgen receptor (AR) inhibitor. Darolutamide inhibits testosterone-induced nuclear translocation of AR. Darolutamide also blocks the activity of the tested mutant ARs arising in response to antiandrogen therapies, including the F876L mutation that confers resistance to enzalutamide and ARN-509. In addition, Darolutamide reduces the growth of AR-overexpressing VCaP prostate cancer cells both in vitro and in a castration-resistant VCaP xenograft model. Darolutamide overcomes resistance to AR-targeted therapies by antagonizing both overexpressed and mutated ARs.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 398.85
Formula C19H19ClN6O2
CAS Number 1297538-32-9
Purity >99%
Solubility DMSO ≥ 60 mg/mL
Storage at -20°C
References

[1] Jiang Yu, et al. Eur J Med Chem. Discovery and biological evaluation of darolutamide derivatives as inhibitors and down-regulators of wild-type AR and the mutants

[2] Tatsuo Sugawara, et al. Int J Cancer. Darolutamide is a potent androgen receptor antagonist with strong efficacy in prostate cancer models

[3] Anu-Maarit Moilanen, et al. Sci Rep. Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Darolutamide, ODM-201; BAY-1841788 supplier, Androgen Receptor, inhibitors

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