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AZ13824374

Cat. No. M21069
AZ13824374  Structure
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Quality Control & Documentation
Biological Activity

AZ13824374 is an in vitro ATAD2 inhibitor with anti-proliferative activity against breast cancer. pIC50 of AZ13824374 against ATAD2 in the ATAD2 FRET and ATAD2 NanoBRET assays were 8.2 and 6.2, respectively.

Chemical Information
Molecular Weight 562.68
Formula C30H39FN8O2
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] Jiahui Fu, et al. Theranostics. ATPase family AAA domain-containing protein 2 (ATAD2): From an epigenetic modulator to cancer therapeutic target

[2] Jon J Winter-Holt, et al. J Med Chem. Discovery of a Potent and Selective ATAD2 Bromodomain Inhibitor with Antiproliferative Activity in Breast Cancer Models

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  Catalog
Abmole Inhibitor Catalog




Keywords: AZ13824374 supplier, Epigenetic Reader Domain, inhibitors, activators


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