528100

PI-103

A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR.

• Synonyme(s) : PI-103, 3-(4-(4-Morpholinyl)pyrido[3ʹ,2ʹ:4,5]furo[3,2-d]pyrimidin-2-yl)phenol, mTOR Inhibitor V, PI 3-K Inhibitor V
• Formule empirique (notation de Hill) : C₁₉H₁₆N₄O₃
• CAS Number: 371935-74-9
• Poids moléculaire : 348.36
• Numéro MDL: MFCD11983145
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Essai: ≥97% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: white
• Solubilité: DMSO: 5 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C
• Chaîne SMILES: N5(CCOCC5)c1nc(nc3c1[o]c4ncccc43)c2cc(ccc2)O
• InChI: 1S/C19H16N4O3/c24-13-4-1-3-12(11-13)17-21-15-14-5-2-6-20-19(14)26-16(15)18(22-17)23-7-9-25-10-8-23/h1-6,11,24H,7-10H2
• Clé InChI: TUVCWJQQGGETHL-UHFFFAOYSA-N

Description

Description générale

A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR (IC₅₀ = 2, 8, 88, 48, 150, 26, 20, and 83 nM for DNA-PK, p110α, p110β, p110δ, p110γ, PI3-KC2β, mTORC1, and mTORC2, respectively). It inhibits ATR and ATM only at much higher concentrations (IC₅₀ = 850 and 920 nM, respectively) and exhibits little activity towards a panel of more than 40 other kinases even at concentrations as high as 10 µM. Shown to effectively block PI3-K/Akt signaling and cell proliferation in glioma cell lines both in vitro and in vivo. A 10 mM (2 mg/574 µl) solution of PI-103 (Cat. No. 528101) in DMSO is also available.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
DNA-PK, PI3-K, and mTOR

Product competes with ATP.

Reversible: no

Target IC₅₀: 2, 8, 88, 48, 150, 26, 20, and 83 nM for DNA-PK, p110α, p110β, p110delta;, p110γ, PI3-KC2β, mTORC1, and mTORC2, respectively

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Notes préparatoires

Slight warming may be required for complete solubilization.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable