PQR620
PQR620 Basic information
- Product Name:
- PQR620
- 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)-
- mTOR,PQR-620,PQR 620,PQR620,Mammalian target of Rapamycin,Inhibitor,inhibit
- 5-(4,6-Di((1R,5S)-3-oxa-8-azabicyclo[3.2.1]octan-8-yl)-1,3,5-triazin-2-yl)-4-(difluoromethyl)pyridin-2-amine
- 5-[4,6-Bis(3-oxa-8-azabicyclo[3.2.1]oct-8-yl)-1,3,5-triazin-2-yl]-4-(difluoromethyl)-2-pyridinamine
- PQR620, 10 mM in DMSO
- CAS:
- 1927857-56-4
- MF:
- C21H25F2N7O2
- MW:
- 445.47
- Mol File:
- 1927857-56-4.mol
PQR620 Chemical Properties
- 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
PQR620 Usage And Synthesis
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
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.
PQR620Supplier
- Tel
- 025-83697070
- info@chemlin.com.cn
- Tel
- 028-81700200 18116577057
- 3003855609@qq.com
- Tel
- 13621943973
- sales@shjiyipharmatech.com
- Tel
- 021-52996696，15000506266 15000506266
- Tel
- 021-61312847; 18021002903
- 3008007409@qq.com