TG100-115

SKU: orb1305184

Description

TG100-115

Research Area

Signal Transduction

Key Properties

• CAS Number: 677297-51-7
• MW: 346.34
• Purity: 98.95%
• Formula: C₁₈H₁₄N₆O₂
• SMILES: Nc1nc(N)c2nc(-c3cccc(O)c3)c(nc2n1)-c1cccc(O)c1
• Target: PI3K
• Solubility: DMSO:40 mg/mL (115.49 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.77 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  PI3Kδ:235 nM|PI3Kγ:83 nM
• In Vivo:
  In human umbilical vein endothelial cells, TG100-115 (10 μM) did not affect cell proliferation and VEGF-stimulated ERK phosphorylation, but blocked other vascular endothelial growth factor (VEGF) signaling pathways, such as VE-calmodulin phosphorylation, and thus inhibited the overall increase in the level of VE-calmodulin induced by VEGF. TG100-115 (0.125-10 μM) also inhibited FGF-stimulated Akt phosphorylation.The inhibitory effect of TG100-115 on PI3Kα/β was weak (IC50: 1.2/1.3 mM).TG100-115 inhibited vascular endothelial growth factor-regulated phosphorylation of p70S6 and mTOR kinase.
• In Vitro:
  In human umbilical vein endothelial cells, TG100-115 (10 μM) did not affect cell proliferation and VEGF-stimulated ERK phosphorylation, but blocked other vascular endothelial growth factor (VEGF) signaling pathways, such as VE-calmodulin phosphorylation, and thus inhibited the overall increase in the level of VE-calmodulin induced by VEGF. TG100-115 (0.125-10 μM) also inhibited FGF-stimulated Akt phosphorylation.The inhibitory effect of TG100-115 on PI3Kα/β was weak (IC50: 1.2/1.3 mM).TG100-115 inhibited vascular endothelial growth factor-regulated phosphorylation of p70S6 and mTOR kinase.
• Cell Research:
  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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, Phosphoinositide 3-kinase, PI3Kγ, PI3Kδ, PI3Kβ, PI3Kα, PI3K, TG100 115, TG100115, TG-100-115, TG100-115

Compound Identifiers

PubChem CID

10427712