PIK-90 is a novel and potent PI3K inhibitor with IC50 values of 11 nM, 350 nM, 18 nM and 58 nM for p110α, p110β, p110γ and p110δ respectively. Phosphoinositide 3-kinases (PI3Ks) are among the most frequently activated signaling pathways in cancer. Inhibition with p110alpha inhibitor PIK-90 resulted in a significant reduction of chemotaxis and actin polymerization to CXCL12 and reduced migration beneath MSC (pseudoemperipolesis). In suspension and MSC cocultures, PIK-90 was potent inducers of CLL cell apoptosis.
|Cell lines||LN229:EGFR (PTENwt) and U87:EGFR (PTENmt) cells|
|Preparation method||Cell proliferation assay and flow cytometry. For viability, 105 cells were seeded in 12-well plates in the presence of erlotinib, PI-103, PIK-90, rapamycin, erlotinib plus PIK-90, erlotinib plus rapamycin, erlotinib plus PIK-90, and rapamycin or erlotinib plus PI-103 for 72 h. Cell viability was determined using a WST-1 assay (Roche Molecular Biochemicals).|
|Concentrations||0, 0.1, 0.5, 1µM|
|Animal models||Human primary GBM43 cells female BALB/c nu/nu mice bearing xenografts model|
|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.
|Source||Proc Natl Acad Sci U S A (2012). Figure 1.PIK-90|
|Cell Lines||PTENWT and PTENMT glioma cell lines|
|Incubation Time||24 h|
|Results||Like PIK-90, PI-103, and LY294002, PIK-75 could block phosphorylation of Akt|
Isoform-selective phosphoinositide 3'-kinase inhibitors inhibit CXCR4 signaling and overcome stromal cell-mediated drug resistance in chronic lymphocytic leukemia: a novel therapeutic approach.
Niedermeier M, et al. Blood. 2009 May 28;113(22):5549-57. PMID: 19318683.
|Related PI3K Products|
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.
GNE-317 is a potent, brain-penetrant PI3K inhibitor.
Serabelisib (INK-1117,MLN-1117,TAK-117) is a potent and selective oral PI3Kα isoform inhibitor (IC50 of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinase.
SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
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