CNX-1351 potently inhibited PI3Kα and was 20−400 times less potent against β, γ, and δ. CNX-1351 inhibits PI3Kα signaling in cells and shows prolonged inhibition consistent with a covalent mechanism of Action. CNX-1351 inhibits growth of cells dependent on PI3Kα. CNX-1351 also inhibits PI3Kα signaling in vivo and bonds to p110α.
|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.
Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα.
Nacht M, et al. J Med Chem. 2013 Feb 14;56(3):712-21. PMID: 23360348.
|Related PI3K Products|
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.
IPI-3063 is a potent and selective p110δ inhibitor with biochemical IC50 of 2.5 ± 1.2 nM and IC50 values for the other class I PI3K isoforms (p110α, p110β, p110γ) are at least 400-fold higher.
GDC-0084 is a brain penetrant inhibitor of PI3K and mTOR.
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