| 產(chǎn)品描述： | PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar Kd toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity |
| 靶點(diǎn)： |
mTOR:0.33 nM (Kd);PI3Kα:0.84 nM (Kd);PI3Kβ:6.1 nM (Kd);PI3Kγ:10 nM (Kd);PI3Kδ:11 nM (Kd);PI3KC2β:100 nM (Kd);PI3K;?mTOR |
| 體外研究： |
PQR-530 is a potent, oral and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, exhibiting antitumor activity. PQR-530 inhibits all PI3K isoforms and mTOR complexes C1/2 potently and selectively. PQR-530 inhibits protein kinase B (PKB, pSer473) and ribosomal protein S6 (pS6, pSer235/236) phosphorylation with IC50 values of 0.07 μM in A2058 melanoma cells. PQR-530 shows inhibitory activity against the growth of 44 cancer cell lines with mean GI50 of 426 nM |
| 參考文獻(xiàn)： |
1. Denise Rageot, et al. Abstract 140: Discovery and biological evaluation of PQR530, a highly potent dual pan-PI3K/mTORC1/2 inhibitor. Cancer Res 2017;77(13 Suppl). 2. Rageot D, et al. (S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase. J Med Chem. 2019;62(13):6241-62 |
| 溶解性： |
Soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.454 ml |
12.272 ml |
24.544 ml |
| 5 mM |
0.491 ml |
2.454 ml |
4.909 ml |
| 10 mM |
0.245 ml |
1.227 ml |
2.454 ml |
| 50 mM |
0.049 ml |
0.245 ml |
0.491 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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