TGX-221

Catalog No.S1169

For research use only.

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.

TGX-221 Chemical Structure

CAS No. 663619-89-4

Selleck's TGX-221 has been cited by 83 publications

Purity & Quality Control

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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 MULGeY5kfGmxbjDBd5NigQ>? MUK1NFDDqG6P MYexJIg> NWfBboQ{TE2VTx?= M2nuNZJm\HWlZYOgRYt1KHCqb4PwbI9zgWyjdHnvci=> NIjLXYgzOjhzNEG3NC=>
DU145 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnybIUyUUN3ME2zOU43KMLzIECuNVIh|ryP NGTZfnYzOjR7NES0OC=>
PC3 NX\sflN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HIWGlEPTB;MUiuNkDDuSByLki1JO69VQ>? M1Gzc|IzPDl2NES0
LNCaP MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17QS2lEPTB;Mz65PEDDuSByLkG4JO69VQ>? M{P0Z|IzPDl2NES0
Assay
Methods Test Index PMID
Growth inhibition assay Cell viability 27176481
Western blot p-AKT / AKT ; phospho-Zyxin / Zyxin / p-FAK / FAK 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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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]
  • 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 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CN2C(=O)C=C(N=C2C(=C1)C(C)NC3=CC=CC=C3)N4CCOCC4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

Handling Instructions

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