CPI-1612 is a tool compound that appears to be a fairly efficient EP300/CBP histone acetyltransferase (HAT) inhibitor, exhibiting activity in xenograft models with good PK of higher species.
|Solubility (25°C)||DMSO ≥ 60 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Related Histone Acetyltransferase Products|
KAT modulator-1 is a KAT modulator.
KAT6-IN-1 is a potent KAT6 inhibitor.
MC4171 is a selective KAT8 inhibitor (IC50=8.1 µM).
MOZ-IN-3 is a KAT6A (MOZ) acetyltransferase inhibitor (IC50: 30 nM).
Ep300/CREBBP-IN-4 is a potent Ep300 and CREBBP inhibitor with IC50s of 0.024 and 0.064 μM, respectively.
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