TG100-115 is a potent small molecule PI3K γ/δ inhibitor potently inhibited edema and inflammation in response to multiple mediators known to participate in myocardial infarction, including vascular endothelial growth factor and platelet-activating factor. TG100-115, inhibited PI3Kγ and -δ (IC50 values of 83 and 235 nM, respectively), whereas both PI3Kα and -β were relatively unaffected (IC50 values >1 μM). TG100-115 also blocked histamine-induced permeability, as predicted based on PI3K's role in GPCR signaling. Additionally, TG100-115 did not block VEGF-induced angiogenesis in vivo.
 |
Source | Cancer Discov (2016). Figure 4.TG100-115 |
| Method | i.v. | |
| Cell Lines | WT mice | |
| Concentrations | 10 mg/kg | |
| Incubation Time | 48 hours | |
| Results | Intravital imaging revealed that control-treated mice exhibited large pancreatic tumors and multiple metastases, whereas TG100-115–treated mice had signifi cantly smaller pancreatic tumors and few, if any, metastases |
| Cell Experiment | |
|---|---|
| Cell lines | Human umbilical vein EC |
| Preparation method | Cell proliferation assay. Human umbilical vein EC plated in 96-well cluster plates (5,000 cells/well) were cultured in assay medium (containing 0.5% serum and 50 ng/ml VEGF) in the presence or absence of test compounds (10 μM), and cell numbers were quantified by XTT assay (Promega, Madison, WI) 24, 48, or 72 h later. |
| Concentrations | 10 μM |
| Incubation time | 24, 48, or 72 h |
| Animal Experiment | |
|---|---|
| Animal models | Rodent and porcine MI models |
| Formulation | either PEG or sulfobutyl ether β-cyclodextrin (CyDex, Lenexa, KS) formulations |
| Dosages | 0.5mg/kg or 1mg/kg |
| Administration | i.v. at 0–3 h after reperfusion |
| Molecular Weight | 346.34 |
| Formula | C18H14N6O2 |
| CAS Number | 677297-51-7 |
| Solubility (25°C) | DMSO 9 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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