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ONT-993

Cat. No. M42318
ONT-993 Structure
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Biological Activity

ONT-993 is an aliphatic hydroxylated metabolite.

Chemical Information
Molecular Weight 496.52
Formula C26H24N8O3
CAS Number 937263-81-5
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] Ariel R Topletz-Erickson et al. Clin Pharmacokinet. The Pharmacokinetics and Safety of Tucatinib in Volunteers with Hepatic Impairment

[2] Ariel Topletz-Erickson et al. Clin Pharmacokinet. Evaluation of Safety and Clinically Relevant Drug-Drug Interactions with Tucatinib in Healthy Volunteers

[3] Hao Sun et al. Cancer Chemother Pharmacol. Elimination of tucatinib, a small molecule kinase inhibitor of HER2, is primarily governed by CYP2C8 enantioselective oxidation of gem-dimethyl

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  Catalog
Abmole Inhibitor Catalog




Keywords: ONT-993 supplier, Cytochrome P450 (e.g. CYP17), inhibitors, activators


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