1. PI3K/Akt/mTOR
  2. PI3K

TG100-115 

Cat. No.: HY-10111 Purity: 98.96%
Handling Instructions

TG100-115 is a selective PI3Kγ/PI3Kδ inhibitor with IC50s of 83 and 235 nM, respectively.

For research use only. We do not sell to patients.
TG100-115 Chemical Structure

TG100-115 Chemical Structure

CAS No. : 677297-51-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 106 In-stock
5 mg USD 96 In-stock
10 mg USD 156 In-stock
50 mg USD 468 In-stock
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

TG100-115 is a selective PI3Kγ/PI3Kδ inhibitor with IC50s of 83 and 235 nM, respectively.

IC50 & Target

IC50: 83 nM (PI3Kγ), 235 nM (PI3Kδ)[1]

In Vitro

TG100-115 inhibits PI3Kγ and PI3Kδ with IC50s of 83 and 235 nM, respectively, whereas both PI3Kα and PI3Kβ are relatively unaffected (IC50 values >1 μM). As a gauge of general specificity, TG100-115 is also assayed against a 133 protein kinase panel, none of which are inhibited at IC50 values <1 μM. TG100-115 potently inhibits edema and inflammation in response to multiple mediators known to participate in myocardial infarction, including vascular endothelial growth factor and platelet-activating factor; by contrast, endothelial cell mitogenesis, a repair process important to tissue survival after ischemic damage[1].

In Vivo

To correlate these in vivo responses with the molecular target of interest, PI3K pathway signaling is monitored through western blot analyses of Akt phosphorylation (a PI3K-mediated event). VEGF injection i.v. in mice induces a rapid Akt phosphorylation readily detectable in lung lysates, pretreatment with TG100-115 blocks this response. Blockade is seen with TG100-115 doses as low as 0.5 mg/kg and persists over a period of several hours. In initial dose-ranging studies, generally equivalent responses are observed using TG100-115 doses of 0.5-10 mg/kg, and we therefore elected to conduct a statistically powered test at the lowest dose. Animals dosed with TG100-115 as a single 0.5 mg/kg i.v. bolus 30 min after reperfusion developed smaller infarcts vs. vehicle-treated controls. Measuring infarct area as percent of total LV ischemic area, infarct size is reduced by 35% (P=0.04). Viable tissue within the ischemic zone is increased by 37% (P=0.04), directly demonstrating the cardioprotective effect of PI3Kγ/δ inhibition[1].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.8873 mL 14.4367 mL 28.8734 mL
5 mM 0.5775 mL 2.8873 mL 5.7747 mL
10 mM 0.2887 mL 1.4437 mL 2.8873 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

PI3K reactions are constructed by using recombinant human kinases, 3 μM ATP, phosphatidylinositol substrate, and cofactors, and reaction progression measured by using a luminescent-based detection system to quantify ATP consumption. Protein kinase assays are performed by using commercial screening services[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

TG100-115 is prepared in DMSO and then diluted with appropriate medium[1].

Human umbilical vein EC plated in 96-well cluster plates (5,000 cells/well) are cultured in assay medium (containing 0.5% serum and 50 ng/mL VEGF) in the presence or absence of test compounds (e.g., TG100-115) (10 μM), and cell numbers are quantified by XTT assay 24, 48, or 72 h later[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

TG100-115 is prepared for in vivo assays as either PEG or sulfobutyl ether β-cyclodextrin formulations[1].

Rats[1]
Sprague-Dawley rats (175-200 g) are dosed i.v. with either TG100-115 (1 mg/kg) or vehicle, and 1-4 h later Evans blue dye is administered i.v. as 500 μl of a 2% sterile saline solution. Immediately after dye injection, animals are injected intradermally on each shaved flank with 100 μL of saline, VEGF (2 μg/mL stock), or histamine (10 μg/mL stock). Thirty minutes later, injection sites are photographed.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

346.34

Formula

C₁₈H₁₄N₆O₂

CAS No.

677297-51-7

SMILES

NC1=C(C(N=C2C3=CC(O)=CC=C3)=NC(N)=N1)N=C2C4=CC(O)=CC=C4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 5.45 mg/mL (Need ultrasonic and warming)

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.96%

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Product Name:
TG100-115
Cat. No.:
HY-10111
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