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PI-103

Cat. No. M1773
PI-103 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 140 In stock
50mg USD 350 In stock
100mg USD 450 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 348.36
Formula C19H16N4O3
CAS Number 371935-74-9
Purity >98%
Solubility DMSO
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PI-103 supplier, PI3K, inhibitors

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