产品说明书

PQR620

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Chemical Structure| 1927857-56-4 同义名 : -
CAS号 : 1927857-56-4
货号 : A692574
分子式 : C21H25F2N7O2
纯度 : 99%+
分子量 : 445.466
MDL号 : MFCD30489733
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 5 mg/mL(11.22 mM)，配合水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 PQR620 is recognized as an orally bioavailable, brain-penetrant inhibitor with selectivity for mTORC1/2. It is a potent mTOR inhibitor, showing over 1000-fold selectivity against PI3Kα in binding assays. In A2058 melanoma cells, PQR620 inhibits phosphorylation of protein kinase B (pSer473) and ribosomal protein S6 (pSer235/236) with IC50 values of 0.2 μM and 0.1 μM, respectively. It also displays remarkable selectivity across a broad spectrum of kinases, unrelated receptor enzymes, and ion channels. PQR620's efficacy in halting cancer cell proliferation is demonstrated in an NTRC 44 cancer cell line panel[1]. When tested on 44 lymphoma cell lines, PQR620 has a median IC50 of 250 nM, showing greater activity in B cell tumors compared to T cell tumors (median IC50s: 250 nM vs 450 nM). After 72 hours, PQR620's anti-tumor activity is primarily cytostatic, with apoptosis observed in only 6 out of 44 cell lines (13%). Sensitivity to PQR620 and apoptosis induction are consistent between DLBCL and MCL, unaffected by the DLBCL cell of origin, TP53 status, or the presence of MYC or BCL2 translocations[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.24mL

0.45mL

0.22mL

11.22mL

2.24mL

1.12mL

22.45mL

4.49mL

2.24mL
参考文献

[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.