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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. 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 |
| Related PI3K Products |
|---|
| AS605240
AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) with an IC50 of 8 nM. |
| BEZ235
BEZ235 (NVP-BEZ235) is a potent dual PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively. |
| BKM120 (Buparlisib)
BKM120 (NVP-BKM120) is a potent and highly specific oral pan-class I PI3K inhibitor. |
| GDC-0941 (Pictilisib)
GDC-0941 is a selective and potent inhibitor of Class I PI3K, p110a IC50=0.003uM, U87MG IC50=0.95μM. |
| AS-252424
AS-252424 is a furan-2-ylmethylene thiazolidinedione as a selective ATP-competitive PI3Kγ inhibitor with IC50 with 33 nM. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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