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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.
Cell Commun Signal. 2022 Jul 7;20(1):102.
Circular dorsal ruffles disturb the growth factor-induced PI3K-AKT pathway in hepatocellular carcinoma Hep3B cells
TGX-221 purchased from AbMole
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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. |
| 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 |
| 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 |
| Related PI3K Products |
|---|
| AS605240
AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) with an IC50 of 8 nM. |
| BEZ235
BEZ235 (NVP-BEZ235) is a potent dual PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively. |
| BKM120 (Buparlisib)
BKM120 (NVP-BKM120) is a potent and highly specific oral pan-class I PI3K inhibitor. |
| GDC-0941 (Pictilisib)
GDC-0941 is a selective and potent inhibitor of Class I PI3K, p110a IC50=0.003uM, U87MG IC50=0.95μM. |
| AS-252424
AS-252424 is a furan-2-ylmethylene thiazolidinedione as a selective ATP-competitive PI3Kγ inhibitor with IC50 with 33 nM. |
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