- 貨號 Cat. No.
- S1352
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
TG100-115
TG100115 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 |
|
|---|
10mM/1mLIn DMSO |
USD 302 |
In stock |
0
1
2
3
4
5
6
7
8
9
10
|
5mg |
USD 214 |
In stock |
0
1
2
3
4
5
6
7
8
9
10
|
10mg |
USD 340 |
In stock |
0
1
2
3
4
5
6
7
8
9
10
|
50mg |
USD 970 |
In stock |
0
1
2
3
4
5
6
7
8
9
10
|
100mg |
USD 1600 |
In stock |
0
1
2
3
4
5
6
7
8
9
10
|
|
Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
Description |
TG100115 is a PI3Kγ/δ inhibitor with IC50 of 83 nM/235 nM, with little effect on PI3Kα/β. Phase 1/2. |
|---|
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] |
|---|
Features |
A potent and dual selective PI3Kγ/δ inhibitor. |
|---|
Protocol(Only for Reference)
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 late |
|---|
Animal Study: [1]
Animal Models |
Rat (Sprague-Dawley) myocardial ischemia (MI) model |
|---|
Dosages |
0.5-5 mg/kg |
|---|
Administration |
By intravenous injection. |
|---|
1
References
Clinical Trial Information( data from http://clinicaltrials.gov)
NCT Number |
Recruitment |
Conditions |
Sponsor
/Collaborators |
Start Date |
Phases |
|---|
NCT00103350 |
Completed |
Myocardial Infarction |
TargeGen |
2005-01 |
Phase 1|Phase 2 |
Download TG100-115 SDF
Molecular Weight (MW) |
346.34 |
|---|
Formula |
C18H14N6O2
|
|---|
CAS No. |
677297-51-7 |
|---|
Storage |
3 years -20℃Powder |
|---|
6 months-80℃in DMSO |
Syonnyms |
N/A |
|---|
Solubility (25°C) * |
In vitro |
DMSO |
9 mg/mL (25 mM) |
|---|
Water |
<1 mg/mL (<1 mM) |
Ethanol |
<1 mg/mL (<1 mM) |
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name |
6,7-Bis(3-hydroxyphenyl)pteridine-2,4-diamine |
|---|
Stock Solution (1ml DMSO) |
1mM |
10mM |
20mM |
30mM |
|---|
Mass(mg) |
0.34634 |
3.4634 |
6.9268 |
- |
Customer Reviews (1)
Click to enlarge |
Rating |
|
Source |
Saraswati Sukumar of Johns Hopkins University School of Medicine. TG100-115 purchased from Selleck |
Method |
Western blot |
Cell Lines |
T47D cells |
Concentrations |
|
Incubation Time |
1 h |
Results |
TG100-115 treatment resulted in a reduction of AKT phosphorylation in T47D cells. |
詢價 / 洽詢此產品
