SML1239

XL388

≥98% (HPLC)

• Synonyme(s) : XL-388, [7-(6-Amino-3-pyridinyl)-2,3-dihydro-1,4-benzoxazepin-4(5H)-yl][3-fluoro-2-methyl-4-(methylsulfonyl)phenyl]-methanone
• Formule empirique (notation de Hill): C₂₃H₂₂FN₃O₄S
• Numéro CAS: 1251156-08-7
• Poids moléculaire : 455.50
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: powder
• Couleur: white to beige
• Solubilité: DMSO: 5 mg/mL, clear (warmed)
• Température de stockage: −20°C
• InChI: 1S/C23H22FN3O4S/c1-14-18(5-7-20(22(14)24)32(2,29)30)23(28)27-9-10-31-19-6-3-15(11-17(19)13-27)16-4-8-21(25)26-12-16/h3-8,11-12H,9-10,13H2,1-2H3,(H2,25,26)
• Clé InChI: LNFBAYSBVQBKFR-UHFFFAOYSA-N

Description

Actions biochimiques/physiologiques

XL388 is a potent, selective, orally bioavailable ATP-competitive inhibitor of mammalian target of rapamycin (mTOR) with an IC₅₀ of 9.9 nM for mTOR, 8 nM for mTORC1, 166 nM for mTORC2, and 1000-fold selectivity for mTOR over the closely related PI3K kinases and a panel of 141 protein kinases tested. XL388 blocked mTORC1 phosphorylation of p70S6K (T389) with an IC₅₀ value of 94 nM and blocked mTORC2 phosphorylationof AKT (S473) with an IC₅₀ value of 350 nM. XL388 showed complete tumor growth inhibition in mice bearing MCF-7 xenograft tumors.

Informations sur la sécurité

• Pictogrammes: GHS07
• Mention d'avertissement: Warning
• Mentions de danger: H315 - H319 - H335
• Conseils de prudence: P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338
• Classification des risques: Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• Organes cibles: Respiratory system
• 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