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ARD-61

Cat. No. M21160
ARD-61  Structure
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Biological Activity

ARD-61 is a potent and specific PROTAC androgen receptor (AR) depressant. ARD-61 effectively and efficiently induces AR and progesterone receptor (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and also effectively inhibits tumor growth in a mouse MDA-MB-453 xenograft model.

Chemical Information
Molecular Weight 1095.78
Formula C61H71ClN8O7S
CAS Number 2316837-08-6
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] Anna R Michmerhuizen, et al. Br J Cancer. Androgen and oestrogen receptor co-expression determines the efficacy of hormone receptor-mediated radiosensitisation in breast cancer

[2] Lijie Zhao, et al. Neoplasia. A highly potent PROTAC androgen receptor (AR) degrader ARD-61 effectively inhibits AR-positive breast cancer cell growth in vitro and tumor growth in vivo

[3] Steven Kregel, et al. Neoplasia. Androgen receptor degraders overcome common resistance mechanisms developed during prostate cancer treatment

[4] Yan Zheng, et al. JAMA. Associations of Weight Gain From Early to Middle Adulthood With Major Health Outcomes Later in Life

[5] Maria Aparecida Marques dos Santos Mezzacappa, et al. J Pediatr Gastroenterol Nutr. Gastric emptying in premature newborns with acute respiratory distress

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