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DBt-10

Cat. No. M43478
DBt-10 Structure
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Biological Activity

DBt-10 is a potent BTK degrader.

Chemical Information
Molecular Weight 1277.97
Formula C68H86ClFN16O6
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] Martin Schröder et al. Nat Commun. DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic- and acquired-degrader resistance

[2] Yang Zhou et al. RSC Adv. In silico studies of ASEM analogues targeting α7-nAChR and experimental verification

[3] Ansel T Hillmer et al. Eur J Nucl Med Mol Imaging. PET imaging of α7 nicotinic acetylcholine receptors: a comparative study of [18F]ASEM and [18F]DBT-10 in nonhuman primates, and further evaluation of [18F]ASEM in humans

[4] Anna Starikov et al. Clin Imaging. 2D mammography, digital breast tomosynthesis, and ultrasound: which should be used for the different breast densities in breast cancer screening?

[5] Ansel T Hillmer et al. Eur J Nucl Med Mol Imaging. PET imaging evaluation of [(18)F]DBT-10, a novel radioligand specific to α7 nicotinic acetylcholine receptors, in nonhuman primates

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