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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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