Home PI3K/Akt/mTOR PI3K inhibitor - Autophagy activator - DNA-PK inhibitor - mTOR inhibitor - Apoptosis related activator PI-103 For research use only.

PI-103

PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. PI-103 induces apoptosis in murine T-cell Lymphoma.

PI-103 Chemical Structure

PI-103 Chemical Structure

CAS No. 371935-74-9

Size Price Stock Quantity
10mM (1mL in DMSO) USD 197 In stock
5mg USD 147 In stock
25mg USD 370 In stock
50mg USD 590 In stock
100mg USD 790 In stock
200mg USD 1370 In stock
1g USD 2990 In stock
Bulk Size Bulk Discount

Free Delivery on orders over USD 500. Order now.
Selleck USA

Tel: (832) 582-8158

sales@selleckchem.com

Purity & Quality Control

PI-103 Related Products

Signaling Pathway

PI3K Signaling Pathways

PI3K Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
UCH-1  Apoptosis Assay 0.1-10 μM 24 h DMSO induces apoptosis 19528441
UCH-1  Growth Inhibition Assay 0.01-10 μM 6 d inhibits proliferation dose dependently 19528441
UCH-1  Function Assay 0-5 μM inhibits the phosphorylation of both AKT and mTOR in a dose-dependent manner 19528441
Click to View More Cell Line Experimental Data

Biological Activity

Description PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. PI-103 induces apoptosis in murine T-cell Lymphoma.
Features The first potent, synthetic mTOR inhibitor.
Targets
p110α [3]
(Cell-free assay)		 p110β [3]
(Cell-free assay)		 p110δ [3]
(Cell-free assay)		 p110γ [3]
(Cell-free assay)		 DNA-PK [3]
(Cell-free assay)		 Click to View More Targets
2 nM 3 nM 3 nM 15 nM 23 nM
In vitro
In vitro

PI-103 potently inhibits both the rapamycin-sensitive (mTORC1) and rapamycin-insensitive (mTORC2) complexes of the protein kinase mTOR. [1] PI-103 inhibits constitutive and growth factor-induced PI3K/Akt, as well as mTORC1 activation. [2] In blast cells, PI-103 inhibits leukemic proliferation, the clonogenicity of leukemic progenitors and induces mitochondrial apoptosis, especially in the compartment containing leukemic stem cells. PI-103 inhibits p110α >200-fold more potently than p110β. PI-103 also potently blocks production of PI(3,4)P2 and PIP3 in adipocytes and PIP3 in myotubes. [2] PI-103 inhibits phosphorylation of Akt with an IC95 100-fold lower than that for LY294002. Strikingly, PI-103 completely protects animals from stimulated decline in blood glucose. PI-103 has additive proapoptotic effects in blast cells and in immature leukemic cells. [2]
Kinase Assay Enzyme Assays
Phosphatidylinositide 3-kinase inhibitory activity was determined using a scintillation proximity assay in the presence of 1 μmol/L ATP. Inhibition of mTOR protein kinase was determined using a TR-FRET-based LanthaScreen method from Invitrogen. Compounds were assayed at a maximum concentration of 10 μmol/L in the presence of 1 μmol/L ATP, and IC50 values were determined using GraphPad Prism software.
Cell Research Cell lines U87MG cells
Concentrations 0.5 μM
Incubation Time 24 hours
Method

U87MG cells are treated with PI-103 for 24 hours. Cell death is 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) is calculated [(experimental value- low control)/(high control -low control) × 100], where the low-control cells are DMSO treated and high-control cells are Triton treated (1% Triton X-100, 30 min, 37 °
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-AKT / AKT / p-S6K / S6K / p-S6 / S6 / p-p38 / p38 p-GSK3 / GSK3 / p-BAD / BAD / p-MDM2 / MDM2 / p-p27 / p27 β-TrCP1 / p-mTOR 18922908
Immunofluorescence autophagosomes / autolysosomes 26814436
Growth inhibition assay Cell viability 25721419
In Vivo
In vivo

When tumors reach 50-100 mm3, animals are randomized and treated with vehicle or PI-103. PI-103 exhibits significant activity, decreasing average tumor size by 4-fold after 18 days. [2] Mice treated with PI-103 have no obvious signs of toxicity premorbidly (based on body weight, food and water intake, activity, and general exam) or at necropsy. Treated tumors display decreased levels of phosphorylated Akt and S6, consistent with blockade of p110α and mTOR. PI-103 treatment is cytostatic to glioma xenografts. [2]
Animal Research Animal Models 6- to 12-week-old Balbc nu/nu mice bearing U87MG:ΔEGFR cells
Dosages 5 mg/kg
Administration Administered via i.p.

Chemical Information & Solubility

Molecular Weight 348.36 Formula

C19H16N4O3
CAS No. 371935-74-9 SDF Download PI-103 SDF
Smiles C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 24 mg/mL ( (68.89 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator
Clear solution
5%DMSO 40% 5% 50%ddH2O
1.0mg/ml (2.87mM) Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy PI-103 | PI-103 supplier | purchase PI-103 | PI-103 cost | PI-103 manufacturer | order PI-103 | PI-103 distributor