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PI3Kα-IN-4

Name: PI3Kα-IN-4
Brand: TargetMol
SKU: T35527
Rating: 4.5 (1 reviews)

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Catalog No. T35527Cas No. 2322293-83-2

Alias PI3Kα-IN-4

PI3Kα-IN-4 is a potent, selective, and orally active PI3Kα inhibitor with an IC50 of 1.8 nM, demonstrating antitumor activity [1].

PI3Kα-IN-4

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Catalog No. T35527Alias PI3Kα-IN-4Cas No. 2322293-83-2

PI3Kα-IN-4 is a potent, selective, and orally active PI3Kα inhibitor with an IC50 of 1.8 nM, demonstrating antitumor activity [1].

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$1,400	6-8 weeks	6-8 weeks
50 mg	$1,820	6-8 weeks	6-8 weeks
100 mg	$2,500	6-8 weeks	6-8 weeks

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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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Product Introduction

Bioactivity

Description	PI3Kα-IN-4 is a potent, selective, and orally active PI3Kα inhibitor with an IC50 of 1.8 nM, demonstrating antitumor activity [1].
Targets&IC50	PI3Kα:1.8 nM (IC50)
In vitro	PI3Kα-IN-4 (compound 10) inhibits PI3Kα, β, δ, and γ in kinase assays with IC50s of 1.8, 271.0, 13.9, and 13.8 nM, respectively, and in cell-based assays with IC50s of 12.1, 1393, 183, and >10000 nM, respectively [1].
In vivo	PI3Kα-IN-4 (compound 10) (30 mg/kg; p.o. once daily for 21 days) achieves 73.0% tumor growth inhibition in mice. It dose-dependently suppresses tumor growth by 62.5% (15 mg/kg), 86.0% (30 mg/kg), and 90.7% (40 mg/kg) when administered orally once daily for 30 days. Time- and dose-dependent inhibition of Akt phosphorylation is observed in vivo (15-40 mg/kg; p.o. once daily; 1-4 h). The compound shows high Cmax (mouse 22167, rat 2327 nM) and good bioavailability (mouse 59.4%, rat 46.9%) after oral administration (mouse 10, rat 3 mg/kg). Following intravenous injection (mouse 1, rat 1 mg/kg), it has a t1/2 of 0.99 hours in mice and 1.22 hours in rats, with low plasma clearance (mouse 4.16, rat 5.28 mL/min/kg).
Synonyms	PI3Kα-IN-4

Chemical Properties

Molecular Weight	560
Formula	C₂₅H₂₃ClFN₅O₅S
Cas No.	2322293-83-2
Smiles	CNC(=O)[C@H](C)Cn1cnc2ccc(cc2c1=O)-c1cnc(OC)c(NS(=O)(=O)c2ccc(F)cc2Cl)c1

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (178.57 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (5.89 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7857 mL	8.9286 mL	17.8571 mL	89.2857 mL
5 mM	0.3571 mL	1.7857 mL	3.5714 mL	17.8571 mL
10 mM	0.1786 mL	0.8929 mL	1.7857 mL	8.9286 mL
20 mM	0.0893 mL	0.4464 mL	0.8929 mL	4.4643 mL
50 mM	0.0357 mL	0.1786 mL	0.3571 mL	1.7857 mL
100 mM	0.0179 mL	0.0893 mL	0.1786 mL	0.8929 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