TGX-221

For research use only.

Catalog No.S1169

72 publications

TGX-221 Chemical Structure

CAS No. 663619-89-4

TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM in a cell-free assay, 1000-fold more selective for p110β than p110α.

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10mM (1mL in DMSO) CAD 154 In stock
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Selleck's TGX-221 has been cited by 72 publications

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Biological Activity

Description TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM in a cell-free assay, 1000-fold more selective for p110β than p110α.
Targets
p110β [5]
(Cell-free assay)		 p110δ [5]
(Cell-free assay)
5 nM 0.1 μM
In vitro

The activity of TGX-221 against different isoforms is measured in an in vitro PI3K assay using multiple preparations of recombinant p85/p110. TGX-221 show slow potent to p110δ with IC50 of 211 nM. Furthermore, TGX-221 partially attenuates insulin-induced phosphorylation of Ser473 of PKB in J774.2 macrophage cells. [1] TGX-221 inhibits platelet-ECC interaction, platelet aggregation and platelet-granulocyte binding in an extracorporeal circulation (ECC) model. [2] A recent study shows that after treatment with TGX-221 (0.2, 2, and 20 μM), PC3 cells show inhibition of proliferation with a significant reduction of the activity of the p110β PI3K isoform. [3]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HUVECs M1jRT2Z2dmO2aX;uJGF{e2G7 MXO1NFDDqG6P NHfFdoQyKGh? NU\0WnpYTE2VTx?= M1G0epJm\HWlZYOgRYt1KHCqb4PwbI9zgWyjdHnvci=> MkLJNlI5OTRzN{C=
DU145 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\zZ2lEPTB;M{WuOkDDuSByLkGyJO69VQ>? MY[yNlQ6PDR2NB?=
PC3 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm[xTWM2OD1zOD6yJOKyKDBwOEWg{txO MViyNlQ6PDR2NB?=
LNCaP NVHvcnJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIT5TpNKSzVyPUOuPVghyrFiMD6xPEDPxE1? MV2yNlQ6PDR2NB?=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 27176481     


U-87 MG cells were treated with TGX-221 at different concentrations for 48 h. DMSO was used as a carrier control. TGX-221 had no significant inhibitory effect on the cell viability of U-87 MG cells.

27176481
Western blot
p-AKT / AKT ; 

PubMed: 27176481     


TGX-221 dramatically inhibited Akt phosphorylation at Ser473 and Thr308.

phospho-Zyxin / Zyxin / p-FAK / FAK ; 

PubMed: 27176481     


U-87 MG cells were treated with TGX-221 (20 μM) alone and combined with SP600125 (20 μM) for 24 h. Whole cell lysates were separated by SDA-PAGE, and the phosphorylated and total protein levels were determined by Western blotting using antibodies against the corresponding phosphorylated and total proteins. Expression of GAPDH was served as a loading control.

27176481
In vivo As an anti-thrombotic agent, TGX-221 at doses 1 + 1 (49 %) and 3+3 (88 %) improves integrated blood flow over 30 minutes in a mouse model. In addition, Tail bleeding time (BT) (sec) increases with TGX-221 doses of 3 + 3 (median 1560) and 1 + 1 (1305) and mean renal BT (sec) also increases in all TGX-221 groups. [4]

Protocol

Kinase Assay:[1]
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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:[3]
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  • Cell lines: PC3 cells
  • Concentrations: ~20 μM
  • Incubation Time: 24-72 hours
  • Method: 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)
Animal Research:[3]
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  • Animal Models: FeCl3-induced arterial thrombosis in mice
  • Dosages: 0.3 + 0.3, 1 + 1, 3 + 3 mg/kg + mg/kg/hour
  • Administration: Administered via i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 12 mg/mL (32.92 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O
For best results, use promptly after mixing. 		2 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 364.44
Formula

C21H24N4O2
CAS No. 663619-89-4
Storage powder
in solvent
Synonyms N/A
Smiles CC1=CN2C(=O)C=C(N=C2C(=C1)C(C)NC3=CC=CC=C3)N4CCOCC4

In vivo Formulation Calculator (Clear solution)

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID