TG100-115

Catalog No.S1352

TG100-115 Chemical Structure

Molecular Weight(MW): 346.34

TG100-115 is a PI3Kγ/δ inhibitor with IC50 of 83 nM/235 nM, with little effect on PI3Kα/β. Phase 1/2.

Size Price Stock Quantity  
In DMSO USD 240 In stock
USD 170 In stock
USD 270 In stock
USD 770 In stock
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2 Customer Reviews

  • (E) Phosphorylation of CREB affected by different concentrations of TG100-115 determined by using immunoblotting

    Biochim Biophys Acta, 2017, 1861(4):947-957. TG100-115 purchased from Selleck.

    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.

     

     

    Saraswati Sukumar of Johns Hopkins University School of Medicine. TG100-115 purchased from Selleck.

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Description TG100-115 is a PI3Kγ/δ inhibitor with IC50 of 83 nM/235 nM, with little effect on PI3Kα/β. Phase 1/2.
Features A potent and dual selective PI3Kγ/δ inhibitor.
Targets
PI3Kγ [1]
(Cell-free assay)
PI3Kδ [1]
(Cell-free assay)
PI3Kβ [1]
(Cell-free assay)
PI3Kα [1]
(Cell-free assay)
83 nM 235 nM 1.2 μM 1.3 μM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HUVEC cells MVXGeY5kfGmxbjDhd5NigQ>? M1HtbVExKM7:TR?= NIL1PHpKdmirYnn0bY9vKG:oIG\FS2YucW6mdXPl[EBXTS2lYXTo[ZJqdiCyaH;zdIhwenmuYYTpc44hcW5iSGXWSWMh[2WubIOgZpkhX2W|dHXyckBjdG:2IHH0JFExKHWP MUexO|Y5PTZyMh?=

... Click to View More Cell Line Experimental Data

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]

Protocol

Kinase Assay:[1]
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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 Research:[1]
+ Expand
  • 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 late
    (Only for Reference)
Animal Research:[1]
+ Expand
  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 9 mg/mL (25.98 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
5% DMSO+30% PEG 300+ddH2O
0.4mg/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 346.34
Formula

C18H14N6O2

CAS No. 677297-51-7
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00103350 Completed Myocardial Infarction TargeGen January 2005 Phase 1|Phase 2

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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID