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.
Front Oncol. 2022 Jul 28;12:968547.
Comprehensive analysis of the glutathione S-transferase Mu (GSTM) gene family in ovarian cancer identifies prognostic and expression significance
PI-103 purchased from AbMole
Cancer Biol Ther. 2018 May 25;1-20.
Preclinical evaluation of novel PI3K/mTOR dual inhibitor SN202 as potential anti-renal cancer agent
PI-103 purchased from AbMole
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Source | Cancer Biol Ther (2018). Figure 3. PI103 (AbMole BioScience) |
| Method | CCK-8 assay | |
| Cell Lines | RCC 786-0 cell line | |
| Concentrations | 10 mmol/L | |
| Incubation Time | 48 or 72 h | |
| Results | These IC50 values were obviously lower than that of the compounds BEZ235 and BKM120, which may be promising candidates for development as new drugs targeting the PI3K pathway. |
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Source | Oncotarget (2016). Figure 1. PI-103 |
| Method | Western blot | |
| Cell Lines | GaMG, SNB19, SW480 and SW48 cells | |
| Concentrations | 0–20 μM | |
| Incubation Time | 24 h | |
| Results | PI-103 alone did not induce any radiosensitization in all tested cells lines, as evident from the closely overlapping curves 2 and 1 (control) in Figure 1B. |
| Cell Experiment | |
|---|---|
| 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). |
| Concentrations | 0~100 µM |
| Incubation time | 24 hr |
| Animal Experiment | |
|---|---|
| Animal models | U87MG:EGFR cells bearing Balbc nu/nu mice |
| Formulation | 50% DMSO |
| Dosages | 5 mg/kg from the 12th to 29th day |
| Administration | oral |
| Molecular Weight | 348.36 |
| Formula | C19H16N4O3 |
| CAS Number | 371935-74-9 |
| Solubility (25°C) | DMSO 12 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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| Boc-L-cyclobutylglycine
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| PI-273
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| Chaetominine
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