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Apalutamide (ARN-509)

Cat. No. M2270
Apalutamide (ARN-509) Structure
Synonym:

Apalutamide

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 120  USD120 In stock
2mg USD 55  USD55 In stock
5mg USD 90  USD90 In stock
10mg USD 150  USD150 In stock
50mg USD 400  USD400 In stock
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Quality Control & Documentation
Biological Activity

Apalutamide (ARN-509) is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM. ARN-509 inhibits AR nuclear translocation and AR binding to androgen response elements and, unlike bicalutamide, does not exhibit agonist properties in the context of AR overexpression. ARN-509 displayed dose-proportional pharmacokinetics, and demonstrated pharmacodynamic and antitumor activity across all dose levels tested. ARN-509 is currently in a Phase I clinical trial.

Chemical Information
Molecular Weight 477.43
Formula C21H15F4N5O2S
CAS Number 956104-40-8
Solubility (25°C) DMSO 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Rathkopf DE, et al. J Clin Oncol. Phase I study of ARN-509, a novel antiandrogen, in the treatment of castration-resistant prostate cancer.

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