SML1239

XL388

≥98% (HPLC)

• Synonym(e): XL-388, [7-(6-Amino-3-pyridinyl)-2,3-dihydro-1,4-benzoxazepin-4(5H)-yl][3-fluoro-2-methyl-4-(methylsulfonyl)phenyl]-methanone
• Empirische Formel (Hill-System): C₂₃H₂₂FN₃O₄S
• CAS-Nummer: 1251156-08-7
• Molekulargewicht: 455.50
• UNSPSC-Code: 12352200

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 5 mg/mL, clear (warmed)
• Lagertemp.: −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)
• InChIKey: LNFBAYSBVQBKFR-UHFFFAOYSA-N

Beschreibung

Biochem./physiol. Wirkung

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.

Sicherheitshinweise

• Piktogramme: GHS07
• Signalwort: Warning
• H-Sätze: H315 - H319 - H335
• P-Sätze: P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338
• Gefahreneinstufungen: Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• Zielorgane: Respiratory system
• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable