1. PI3K/Akt/mTOR
  2. PI3K
  3. TG100-115

TG100-115 

Cat. No.: HY-10111 Purity: 99.31%
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
Solution
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 106 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 156 In-stock
Estimated Time of Arrival: December 31
50 mg USD 468 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Based on 2 publication(s) in Google Scholar

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Description

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

IC50 & Target

PI3Kγ

83 nM (IC50)

PI3Kδ

235 nM (IC50)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

346.34

Formula

C₁₈H₁₄N₆O₂

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5.45 mg/mL (15.74 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent 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.
References
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]

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]

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