PQR620

SKU: orb1301763

Description

PQR620 is a brain-penetrant small molecule that potently and selectively inhibits both mTORC1 and mTORC2 complexes. This inhibitor is a valuable research tool for studying mTOR signaling in neurological disorders and cancer, applicable in both in vitro biochemical assays and in vivo preclinical models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1927857-56-4
• MW: 445.47
• Purity: 98.11% (May vary between batches)
• Formula: C₂₁H₂₅F₂N₇O₂
• SMILES: [H][C@]12CC[C@]([H])(COC1)N2c1nc(nc(n1)-c1cnc(N)cc1C(F)F)N1[C@@]2([H])CC[C@]1([H])COC2
• Target: mTOR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.24 mM);DMSO:6.4 mg/mL (14.37 mM)

Bioactivity

• In Vivo:
  PQR620 exhibits favorable physico-chemical properties, leading to good oral bioavailability and excellent brain penetration.
• In Vitro:
  PQR620 is a potent and selective mTOR inhibitor with >1000-fold selectivity over PI3Kα in enzymatic binding assays. In A2058 melanoma cells, it inhibits protein kinase B (pSer473) and ribosomal protein S6 (pSer235/236) phosphorylation with IC50 values of 0.2 μM and 0.1 μM, respectively. PQR620 exhibits excellent selectivity across a broad range of kinases, receptor enzymes, and ion channels, and effectively prevents cancer cell growth in the NTRC 44 cancer cell line panel, achieving a 10log(IC50) of 2.86 (nM).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, mTORC1, mTORC2, mTOR, Inhibitor, Mammalian target of Rapamycin, PQR 620, PQR620, PQR-620

Compound Identifiers

PubChem CID

122412735