Research Area
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TG100-115 Chemical Structure
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Biological Activity
| Information | TG100-115 is a potent and dual selective PI3Kγ and -δ inhibitor with IC50 of 83 and 235 nM, respectively. | |||||
|---|---|---|---|---|---|---|
| Targets | PI3Kγ | PI3Kδ | ||||
| IC50 | 83 nM | 235 nM [1] | ||||
| In vitro | TG100-115 inhibits PI3Kγ and -δ, with IC50 of 83 and 235 nM, respectively. TG100-115 is not active for PI3Kα and -β, with IC50 of 1.2 and 1.3 mM. In human umbilical vein endothelial cells (HUVECs), TG100-115 (up to 10 μM) has no effects on cell proliferation and VEGF-stimulated ERK phosphorylation. However, TG100-115 (10 μM) interrupts other VEGF signaling pathways, such as those that culminate in VE-cadherin phosphorylation. [1] In HUVECs, TG100-115 (10 μM) inhibits the VEGF-induced increase of total level of VE-cadherin. TG100-115 inhibits VEGF mediated phosphorylation of mTOR and p70S6 kinase, both of which are downstream of PI3K. TG100-115 (125 nM to 10 μM) also inhibits FGF-stimulated phosphorylation of Akt. [2] | |||||
| In vivo | In Miles assay models, TG100-115 (1–5 mg/kg) reduces edema formation and inflammation in rats. In rigorous rodent and porcine models of myocardial ischemia (MI), TG100-115 (0.5–5 mg/kg) provides potent cardioprotection, limits infarct development, and preserves myocardial function. [1] In mice, TG100-115 (5 mg/kg) markedly diminishes vascular permeability (VP) in response to either Sema3A or VEGF, indicating that both factors may depend on PI3Kγ/δ to induce VP. [3] In a mouse asthma model, aerosolized TG100-115 markedly reduces the pulmonary eosinophilia, inhibits interleukin-13 and mucin accumulation. [4] | |||||
| Clinical Trials | TG100-115 is currently under a Phase I/II clinical trial in myocardial infarction. | |||||
| Features | TG100-115 is a potent and dual selective PI3Kγ/δ inhibitor. | |||||
Protocol
Kinase Assay: [1]
| PI3K assays | Forty mL of reaction buffer (20 mM Tris/4 mM MgCl2/10 mM NaCl, pH 7.4) containing 50 mM D-myo-phosphatidylinositol 4,5-bisphosphate substrate and the desired PI3K isoform are aliquoted to 96-well plates; kinase concentrations are 250-500 ng/well, such that linear kinetics are achieved over 90 min. TG100-115 is then added as 2.5 mL of a DMSO stock to final concentration range of 100 mM to 1 nM. Reactions are initiated by addition of 10 mL of ATP to a final concentration of 3 mM, and after 90 min, 50 mL of Kinase-Glo reagent added to quantify residual ATP levels; luminosity is measured using an Ultra 384 instrument. Control reactions omitting either TG100-115 or substrate are also performed. IC50 values are derived from experimental data by nonlinear curve fitting using Prism Version 4. |
|---|
Cell Assay: [1]
| Cell lines: | Human umbilical vein endothelial cells (HUVECs) |
|---|---|
| Concentrations: | 10 μM, dissolved in DMSO as stock solution |
| Incubation Time: | 24, 48, and 72 hours |
| Method: | Cells plated in 96-well cluster plates (5 × 103 cells/well) are cultured in assay medium (containing 0.5% serum and 50 ng/ml VEGF) in the presence or absence of TG100-115, and cell numbers are quantified by XTT assay 24, 48, or 72 hours later. |
Animal Study:[1]
| Animal Models: | Rat (Sprague-Dawley) myocardial ischemia (MI) model |
|---|---|
| Formulation: | Dissolved in PEG or sulfobutyl ether β-cyclodextrin |
| Dosages: | 0.5–5 mg/kg |
| Administration: | By intravenous injection. |
Chemical Information
| Molecular Weight (WM): | 346.34 |
|---|---|
| Formula: | C18H14N6O2 |
| CAS No.: | 677297-51-7 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥9mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
Notes:
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We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
Data independently produced by Saraswati Sukumar of Johns Hopkins University School of Medicine---TG100-115 purchased from Selleck TG100-115 purchased from Selleck
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We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
|
Data independently produced by Saraswati Sukumar of Johns Hopkins University School of Medicine---TG100-115 purchased from Selleck
We give free samples and rewards to people who would like to provide us useful scientific data(western blot, etc.) > See Details
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