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PI-103

Cat. No. M1773

All AbMole products are for research use only, cannot be used for human consumption.

PI-103 Structure
Synonym:

PI103

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 90  USD90 In stock
5mg USD 80  USD80 In stock
10mg USD 126  USD126 In stock
50mg USD 310  USD310 In stock
100mg USD 400  USD400 In stock
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Quality Control & Documentation
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
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.
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.
Protocol (for reference only)
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
Chemical Information
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
References

[1] Shepherd C, et al. Leukemia. PI3K/mTOR inhibition upregulates NOTCH-MYC signalling leading to an impaired cytotoxic response.

[2] Glassford J, et al. Blood Cancer J. Inhibition of cell cycle progression by dual phosphatidylinositol-3-kinase and mTOR blockade in cyclin D2 positive multiple myeloma bearing IgH translocations.

[3] Yih LH, et al. Toxicol Sci. Inhibition of the heat shock response by PI103 enhances the cytotoxicity of arsenic trioxide.

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  Catalog
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Keywords: PI-103, PI103 supplier, PI3K, inhibitors, activators

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