PI-103 is a potent, ATP-competitive PI3K,cell-permeable,inhibitor.The IC50 values are 2, 8, 20, 26, 48, 83, 88, 150 nM for DNA-PK, p110α, mTORC1, PI3-KC2β, p110δ, mTORC2, p110β, and p110γrespectively.PI-103 can be used to target the three Kinases PIK3CA, MRCKA and PIM1.
|Cell lines||U87MG cells|
|Preparation method||For assessment of cell death, U87MG cells were treated with PI-103 or LY294002 for 24 hr. Cell death was quantified by colorimetric determination of LDH activity using a cytotoxicity detection kit (Roche). Percentage of cell death (mean of three 12-well plates per experimental point) was calculated [(experimental value − low control)/(high control − low control) × 100], where the low-control cells were DMSO treated and high-control cells were Triton treated (1% Triton X-100, 30 min, 37°C).|
|Incubation time||24 hr|
|Animal models||U87MG:EGFR cells bearing Balbc nu/nu mice|
|Dosages||5 mg/kg from the 12th to 29th day|
|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.
PI3K/mTOR inhibition upregulates NOTCH-MYC signalling leading to an impaired cytotoxic response.
Shepherd C, et al. Leukemia. 2012 Oct 5. PMID: 23038273.
Inhibition of cell cycle progression by dual phosphatidylinositol-3-kinase and mTOR blockade in cyclin D2 positive multiple myeloma bearing IgH translocations.
Glassford J, et al. Blood Cancer J. 2012 Jan;2(1):e50. PMID: 22829234.
Inhibition of the heat shock response by PI103 enhances the cytotoxicity of arsenic trioxide.
Yih LH, et al. Toxicol Sci. 2012 Jul;128(1):126-36. PMID: 22496356.
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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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