PIK-294 is a highly selective p110 inhibitor with an IC50 of 3 nM. PI3K contains a m-phenol and a pyrazolopyrimidine core. When PIK-294 is compared to tyrosine kinase–selective pyrazolopyrimidines such as PP20, the two molecules span more than 108 fold in relative target selectivity. PIK-294 is 20- to 60-fold more potent than the parent compound, PIK-293, making PIK-294 one of the most potent p110δ- selective inhibitors that has been reported. PIK-294 also inhibits p110α, p110β, p110γ, DNA-PK and mTOR with IC50 of 9.6, 0.67, 0.2, 48 and >50 µM.
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 90 mg/mL|
|Related PI3K Products|
PIK-III (also known as VPS34-IN2) is a potent and selective inhibitor of VPS34 enzymatic activity, with IC50s of 18 nM and 1.2 μM for VPS34 and PI(3)Kδ, respectively.
LY3023414 is a selective ATP-competitive inhibitor of PI3Kα and mTOR, DNA-PK, and other class I PI3K family members.
SAR405 is a PIK3C3/Vps34 inhibitor with an IC50 of 1.2 nM. SAR405 also is a proximal inhibitor of the autophagy machinery.
Tenalisib (RP6530) is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively.
PI 828 is a pI 3-kinase inhibitor, more potent than LY 294002.
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