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About This Item
Empirical Formula (Hill Notation):
C21H25F2N7O2
CAS Number:
Molecular Weight:
445.47
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
powder
Quality Segment
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
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.).
Storage Class
11 - Combustible Solids
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
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