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TGX-221

Catalog No. T2661 CAS 663619-89-4

Synonyms: TGX221

TGX-221, an effective, specific, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, is utilized for cancer treatment.

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TGX-221, CAS 663619-89-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 32.00
2 mg	In stock	$ 45.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 118.00
25 mg	In stock	$ 229.00
50 mg	In stock	$ 378.00
100 mg	In stock	$ 589.00
500 mg	In stock	$ 1,260.00
1 mL * 10 mM (in DMSO)	In stock	$ 74.00

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Purity: 100%

Purity: 98.98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	TGX-221, an effective, specific, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, is utilized for cancer treatment.
Targets&IC50	p110δ:0.1 μM, p110β:5 nM
In vitro	In mouse models, TGX-221 has been shown to enhance blood flow, prolonging tail bleeding and renal bleeding time.
In vivo	In J774.2 macrophages, TGX-221 inhibits the phosphorylation of Ser473 on PKB induced by insulin. It also impedes platelet-ECC (extracorporeal circulation) interactions, platelet aggregation, and the binding between platelets and granulocytes in an ECC model. Furthermore, in the PC3 cells, TGX-221 (at concentrations of 0.2-20 μM) can suppress cell proliferation and reduce the activity of the p110β subunit of PI3K.
Kinase Assay	Lipid kinase activity : IC50 values are measured using a standard lipid kinase activity with PI as a substrate. (i)100 μM cold ATP is used instead of 10 μM, (ii) the DMSO concentration is 1%, and (iii) [γ-33P]ATP is used instead of [γ-32P]ATP. The TLC plates are quantified using a phosphorimager screen. The reported IC50 values are determined by non-linear regression analysis on the basis of at least three independent experiments repeated across multiple preparations of recombinant protein.
Cell Research	For measurement of proliferation, cells are seeded in triplicate in 96-well culture plates and incubated overnight to allow cell attachment. The cells are incubated with TGX-221 for 24, 48, and 72 hours. At designated time intervals, cells are quantified by a crystal violet staining-based colorimetric assay. Briefly, cells are fixed by addition of 100 μl of 2.5% glutaraldehyde solution and incubated at room temperature for 30 minutes. Plates are washed three times by submersion in PBS solution. Plates are air-dried and stained by addition of 100 μL of 0.1% solution of crystal violet dissolved in deionized water and incubated for 20 minutes at room temperature, excess dye is removed by extensive washing with deionized water, and plates are air-dried prior to bound dye solubilization in 100 μL of 10% acetic acid. The optical density of dye extracts is measured directly in plates using a microplate reader at 570 nm.(Only for Reference)

Synonyms	TGX221
Molecular Weight	364.44
Formula	C21H24N4O2
CAS No.	663619-89-4

Storage

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

Solubility Information

DMSO: 18.2 mg/mL (50 mM)

References and Literature

1. Chaussade C, et al. Biochem J. 2007, 404(3), 449-458. 2. Straub A, et al. Thromb Haemost. 2008, 99(3), 609-615. 3. Lu XY, et al. Appl Microbiol Biotechnol. 2011, 89(5), 1423-1433. 4. Bird JE, et al. Thromb Res. 2011, 127(6), 560-564. 5. Jackson SP, et al. Nat Med. 2005, 11(5), 507-514.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Inhibitor Library Kinase Inhibitor Library Anti-Ovarian Cancer Compound Library Antidepressant Compound Library Oxidation-Reduction Compound Library Anti-Pancreatic Cancer Compound Library Anti-Cancer Metabolism Compound Library Anti-Breast Cancer Compound Library

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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

TGX-221 663619-89-4 PI3K/Akt/mTOR signaling PI3K TGX221 TGX 221 Phosphoinositide 3-kinase Inhibitor inhibit inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.