| Identification | Back Directory | [Name]
PQR620 | [CAS]
1927857-56-4 | [Synonyms]
PQR620
PQR-620;PQR 620
PQR620;PQR-620;PQR 620
2-Pyridinamine, 5-[4,6-bis(3-oxa-8-azabicyclo[3.2.1]oct-8-yl)-1,3,5-triazin-2-yl]-4-(difluoromethyl)- | [Molecular Formula]
C21H25F2N7O2 | [MDL Number]
MFCD30502629 | [MOL File]
1927857-56-4.mol | [Molecular Weight]
445.47 |
| Chemical Properties | Back Directory | [Boiling point ]
706.8±70.0 °C(Predicted) | [density ]
1.403±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 6.4 mg/mL (14.37 mM) | [form ]
Solid | [pka]
5.12±0.10(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
PQR620 is an orally bioavailable and selective brain penetrant inhibitor of mTORC1/2[1]. | [in vivo]
The physico-chemical properties of PQR620 result in good oral bioavailability and excellent brain penetration[1]. The activity of PQR620 as single agent undergoes in vivo evaluation in two DLBCL models, the germinal center B cell type DLBCL (GCB-DLBCL) SU-DHL-6 and the acivated B cell-like DLBCL (ABC-DLBCL) RIVA. Treatments with PQR620 (100 mg/kg dose per day, Qd×7/w) start with 100-150 mm3 tumors and are carried for 14 (SU-DHL-6) or 21 days (RIVA). In both models, PQR620 determines a 2-fold decrease of the tumor volumes in comparison with control, with significant differences in both SU-DHL-6 (D7, D9, D11, D14; P<0.005) and RIVA (D14, D16, D19, D21; P<0.005)[2]. | [IC 50]
mTORC1; mTORC2 | [storage]
Store at -20°C | [References]
[1] Florent Beaufils, et al. Abstract 1336: Structure-activity relationship studies, synthesis, and biological evaluation of PQR620, a highly potent and selective mTORC1/2 inhibitor. Cancer Research; 2016 Apr 16-20.
[2] Chiara Tarantelli, et al. Targeting the PI3K/mTOR Pathway in Lymphoma with PQR309 and PQR620: Single Agent Activity and Synergism with the BCL2 Inhibitor Venetoclax. Blood 2016 128:3017. |
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