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PI3Kα-IN-4

Catalog No. T35527Cas No. 2322293-83-2

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

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

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Product Introduction

Bioactivity

Description	PI3Kα-IN-4 is a potent, selective, and orally active PI3Kα inhibitor, demonstrating an IC50 of 1.8 nM and exhibiting antitumor activity[1].
In vitro	PI3Kα-IN-4 (compound 10) inhibits PI3Kα, β, δ, and γ, with IC50s of 1.8, 271.0, 13.9, and 13.8 nM, respectively in kinase assays[1].PI3Kα-IN-4 inhibits PI3Kα, β, δ, and γ, with IC50s of 12.1,1393, 183, and >10000 nM, respectively in cell based assays[1].
In vivo	PI3Kα-IN-4 (compound 10) (30 mg/kg; p.o. once daily for 21 d) achieves the best efficacy, which could inhibit tumor growth by 73.0% in mice[1].PI3Kα-IN-4 (15-40 mg/kg; p.o. once daily for 30 d) dose dependently suppresses tumor growth by 62.5% (15 mg/kg), 86.0% (30 mg/kg) and 90.7% (40 mg/kg), respectively in mice[1].PI3Kα-IN-4 (15-40 mg/kg; p.o. once daily; 1-4 h) inhibits the phosphorylation of Akt in a dose- and time-dependent manner in vivo[1].PI3Kα-IN-4 shows high Cmax (mouse 22167, rat 2327 nM) and good bioavailability (mouse 59.4%, rat 46.9%) following oral administration (mouse 10, rat 3 mg/kg)[1].PI3Kα-IN-4 shows t1/2 (mouse 0.99, rat 1.22 h) and low plasma clearance (mouse 4.16, rat 5.28 mL/min/kg) following intravenous injection (mouse 1, rat 1 mg/kg)[1].
Alias	PI3Kα-IN-4

Chemical Properties

Molecular Weight	560
Formula	C25H23ClFN5O5S
Cas No.	2322293-83-2

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (178.57 mM)

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 mother liquor preparation method and in vivo formula preparation method:

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

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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

Keywords

PI-3Kα-IN-4PI3Ka-IN-4PI3Kalpha-IN-4PI3Kα IN 4PI3KαIN4