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TGX-221

Name: TGX-221
Brand: Selleck Chemicals
SKU: S1169
Rating: 5 (83 reviews)

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.

CAS No. 663619-89-4

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

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PI3K Signaling Pathway Map

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

Click to View More Cell Line Experimental Data

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)

References

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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. Click to purchase: PEG300 Tween 80	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
Storage	2 years	-80°C	in solvent
Smiles	CC1=CN2C(=O)C=C(N=C2C(=C1)C(C)NC3=CC=CC=C3)N4CCOCC4

Download TGX-221 SDF

In vivo Formulation Calculator (Clear solution)

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:μL Number of animals:

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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
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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.

Handling Instructions

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