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PI3Kα-IN-4

Catalog No. T35527 CAS 2322293-83-2

Synonyms: PI3Kα-IN-4

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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PI3Kα-IN-4, CAS 2322293-83-2

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,400.00
50 mg	6-8 weeks	$ 1,820.00
100 mg	6-8 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

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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].
Targets&IC50	PI3Kα:1.8 nM (IC50)
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].

Synonyms	PI3Kα-IN-4
Molecular Weight	560
Formula	C25H23ClFN5O5S
CAS No.	2322293-83-2

Storage

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

Solubility Information

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

References and Literature

1. Dong J, et, al. Discovery of 3-Quinazolin-4(3 H)-on-3-yl-2, N-dimethylpropanamides as Orally Active and Selective PI3Kα Inhibitors. ACS Med Chem Lett. 2020 Jun 10; 11(7): 1463-1469.

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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

PI3Kα-IN-4 2322293-83-2 PI-3Kα-IN-4 PI3Ka-IN-4 PI3Kalpha-IN-4 PI3Kα IN 4 PI3KαIN4 inhibitor inhibit

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