For research use only.

Catalog No.S1169

74 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.

Selleck's TGX-221 has been cited by 74 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.
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 NEDGT2FHfW6ldHnvckBCe3OjeR?= Mm\HOVAxyqCwTR?= NXvSS3h1OSCq NHH4SYxFVVOR MmDvdoVlfWOnczDBb5QheGixc4Doc5J6dGG2aX;u NWHzU4RHOjJ6MUSxO|A>
DU145 M1LRRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jUeGlEPTB;M{WuOkDDuSByLkGyJO69VQ>? NVXHcWlXOjJ2OUS0OFQ>
PC3 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\KTWM2OD1zOD6yJOKyKDBwOEWg{txO M1vOfFIzPDl2NES0
LNCaP NEP0b3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTNwOUigxtEhOC5zODFOwG0> Mo\kNlI1QTR2NES=

... Click to View More Cell Line Experimental Data

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.

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.

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]


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


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

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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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% DMSO % % Tween 80 % ddH2O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID