Acalisib (GS-9820) inhibits the activity of PI3K, thereby preventing the production of the second messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3), which decreases tumor cell proliferation and induces cell death. Wortmannin, LY294002, GDC0941, IC87114 and Acalisib induced a dramatic retraction of osteoclasts within 15-20 min to 65-75% of the initial area. In contrast, there was no significant retraction in response to vehicle, PIK75, TGX221 or AS252424. Moreover, wortmannin and Acalisib (GS-9820), but not PIK75 or TGX221, disrupted actin belts. Whereas PIK75, TGX221, and Acalisib had no significant effect on basal survival, all blocked RANKL-stimulated survival. PI3K-mediated signaling is often dysregulated in cancer cells; the targeted inhibition of PI3K is designed to preserve PI3K signaling in normal, non-neoplastic cells.
|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.
Effects of isoform-selective phosphatidylinositol 3-kinase inhibitors on osteoclasts: actions on cytoskeletal organization, survival, and resorption.
Shugg RP, et al. J Biol Chem. 2013 Dec 6;288(49):35346-57. PMID: 24133210.
|Related PI3K Products|
Bimiralisib (PQR309) is an orally bioavailable inhibitor of PI3K and mTOR, with potential antineoplastic activity.
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.
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