SML4432

PQR620

≥98% (HPLC)

• Synonym(e): 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine, PQR 620, PQR-620
• Empirische Formel (Hill-System): C₂₁H₂₅F₂N₇O₂
• CAS-Nummer: 1927857-56-4
• Molekulargewicht: 445.47
• UNSPSC Code: 12352200
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: -10 to -25°C

Beschreibung

Biochem/physiol Actions

PQR620 is a brain-penetrant, ATP-competitive, potent and selective mTORC1/2 inhibitor with >3700-fold lower potency toward class class I/III PI3K isoforms (mTOR Kd = 0.27 nM, p110α/β/δ/γ Kd = 1/22/23/18 µM, VPS34 Kd = 27.5 µM) and PI4Kβ (Kd >30 µM). PQR620 effectively inhibits cellular mTOR substrates phosphorylation (IC50 = 190 nM/Akt pS473 and 85.2 nM/S6 pS235/236 in A2058 cells) and exhibits antiproliferation activity in cancer cultures (mean GI50 post 72h = 0.92 µM among 66 cancer lines). PQR620 suppresses human ovarian cancer OVCAR-3 tumor growth in mice (50 mg/kg/d p.o.) and eliminates seizure activity of Tsc1GFAP conditional knockout mice in vivo (100 mg/kg/d p.o.).

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable