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TGX-221

Cat. No. M1795

All AbMole products are for research use only, cannot be used for human consumption.

TGX-221 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 37  USD37 In stock
5mg USD 67  USD67 In stock
10mg USD 117  USD117 In stock
50mg USD 397  USD397 In stock
100mg USD 597  USD597 In stock
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Quality Control & Documentation
Biological Activity

TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β. Inhibition appears to occur at the ATP binding site based on the observed increase in IC50 from 5 to ~50 nM at ATP concentrations of 50 µM and 1 mM, respectively. TGX-221 inhibits PtdIns-(3,4)-P2 production in platelets with an IC50 of 50 nM. Selective inhibition of PI3K p110β results in defective platelet thrombus formation and defines PI3K as a target for antithrombotic therapy.

Product Citations
Customer Product Validations & Biological Datas
Source Mol Pharm (2012). Figure 2. TGX-221
Method Western blot assay
Cell Lines LNCaP cells
Concentrations 2 μM
Incubation Time 30 min
Results As demonstrated by Western blot, TGX-221 and BL05 inhibited phosphorylation of Akt, which in turn indicated the inhibitor of PI3K activity.
Protocol (for reference only)
Cell Experiment
Cell lines BT-474 and HCT-116 cell lines
Preparation method For measurement of proliferation, cells were seeded in triplicate at 2×103 cells/well in 96-well culture plates and incubated overnight to allow cell attachment. The cells were incubated with the TGX221-loaded PHA nanoparticles, empty PHA nanoparticles, or free TGX221 for 24, 48, and 72 h. At designated time intervals, cells were quantified by a crystal violet staining-based colorimetric assay (Kueng et al. 1989). Briefly, cells were fixed by addition of 100 μl of 2.5% glutaraldehyde solution andincubated at room temperature for 30 min. Plates were washed three times by submersion in PBS solution. Plates were air-dried and stained by addition of 100 μl of 0.1% solution of crystal violet dissolved in deionized water and incubated for 20 min at room temperature, excess dye was removed by extensive washing with deionized water, and plates were air-dried prior to bound dye solubilization in 100 μ1 of 10% acetic acid. The optical density of dye extracts was measured directly in plates using a microplate reader (Bio-Rad Laboratories, Inc., UK) at 570 nm.
Concentrations 0.2, 2 and 20 μ M
Incubation time 24, 48, and 72 h
Animal Experiment
Animal models prostate cancer LAPC-4, LNCaP, 22RV1 and C4-2 cellsxenograft tumor in nude mice
Formulation dissolved in polypropylene glycol (PPG)
Dosages 100 mg/kg twice a week for 3 weeks
Administration tail vein injection
Chemical Information
Molecular Weight 364.4
Formula C21H24N4O2
CAS Number 663619-89-4
Solubility (25°C) DMSO 18 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Chen R, et al. Prostate. Nanomicellar TGX221 blocks xenograft tumor growth of prostate cancer in nude mice.

[2] Lu XY, et al. Appl Microbiol Biotechnol. Sustained release of PI3K inhibitor from PHA nanoparticles and in vitro growth inhibition of cancer cell lines.

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Keywords: TGX-221 supplier, PI3K, inhibitors, activators

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