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PIK-75

Name: PIK-75
Brand: TargetMol
SKU: T2667
Price: 38 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2667Cas No. 372196-67-3

PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).

PIK-75

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Purity: 99.98%

Catalog No. T2667Cas No. 372196-67-3

PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$38	In Stock	In Stock
10 mg	$52	In Stock	In Stock
25 mg	$113	-	In Stock
50 mg	$193	-	In Stock
100 mg	$297	-	In Stock
1 mL x 10 mM (in DMSO)	$41	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.98%

Appearance:Solid

Color:White to Yellow

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COA LCMS HNMR

Product Introduction

PIK-75 AI Summary

PIK-75 exhibits potent and diverse bioactivities against multiple targets and isoforms. It demonstrates strong inhibition of various PI3K isoforms, especially PI3Kalpha with an IC50 of 0.5 nM, and significant antiproliferative activity against human NZB5 and NZOV9 cells, with IC50 values of 69.0 nM and 66.0 nM, respectively. The compound also shows antitumor activity against human HCT116 cells xenografted in Rag1 knockout mice, leading to a tumor growth inhibition of 23.2% at 20 mg/kg intraperitoneally administered daily for 14 days but causes a body weight loss of 15.0% at the same dose. It inhibits CDK9/cyclin-T1 with an IC50 of 1.37 nM and displays significant inhibitory activity against other kinases such as FLT3 (IC50 of 5.15 nM), DYRK1A, CLK1, and GSK-3beta, with IC50 values ranging from 1.1 nM to 2589.0 nM. Additionally, PIK-75 has antiviral effects, showing inhibition of SARS-CoV-2 3CL-Pro protease by 19.96% at 20 µM concentration and inhibiting influenza A virus strains with an IC50 of 40.0 nM. Despite exhibiting high cytotoxicity against certain cell lines, it shows selective multi-target engagement, displaying extensive potential for therapeutic applications in targeting signaling pathways, cell cycle regulation, and viral infections..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).
Targets&IC50	p110α:5.8 nM, p110γ:76 nM, DNA-PK:2 nM, PI3KC2α:10 μM, mTORC2:10 μM, p110β:1.3 μM, PI3KC2β:1 μM, ATR:21 μM, hsVPS34:2.6 μM, PI4KIIIβ:50 μM, mTORC1:1 μM, ATM:2.3 μM, p110δ:510 nM

Chemical Properties

Molecular Weight	452.28
Formula	C₁₆H₁₄BrN₅O₄S
Cas No.	372196-67-3
Smiles	CN(\N=C\c1cnc2ccc(Br)cn12)S(=O)(=O)c1cc(ccc1C)[N+]([O-])=O
Relative Density.	1.663 g/cm3

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 4.53 mg/mL (10.02 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2110 mL	11.0551 mL	22.1102 mL	110.5510 mL
5 mM	0.4422 mL	2.2110 mL	4.4220 mL	22.1102 mL
10 mM	0.2211 mL	1.1055 mL	2.2110 mL	11.0551 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc