如何选择mTOR抑制剂？
2020-04-22 · 选用指南 · 百灵威授权转载
mTOR即雷帕霉素靶蛋白，含有两种复合体，分别为mTORC1和mTORC2。因其是重要的真核细胞信号，调节细胞的生长、凋亡、自噬等，mTOR成为肿瘤治疗的新靶点，mTOR抑制剂已应用于实体瘤、器官移植等疾病研究及治疗中。
![图1 mTORC1和mTORC2 <sup>[1]</sup>](/assets/jk-articles-all/5fe75314a25c2b80fb134f80.png)
图1 mTORC1和mTORC2 [1]
mTOR抑制剂选择见下表：
1126271
1009298-09-2
AZD-8055, 98%
Description:
a novel ATP-competitive inhibitor of mTOR kinase with an IC50 of 0.8 nM
a novel ATP-competitive inhibitor of mTOR kinase with an IC50 of 0.8 nM
1239103
1092351-67-1
Torkinib, 98%
Description:
a selective and ATP-competitive mTOR inhibitor with an IC50 of 8 nM,PP242 inhibits both mTORC1 and mTORC2 with IC50s of 30 nM and 58 nM
a selective and ATP-competitive mTOR inhibitor with an IC50 of 8 nM,PP242 inhibits both mTORC1 and mTORC2 with IC50s of 30 nM and 58 nM
1497296
1009298-59-2
Vistusertib, 98%
Description:
a novel mTOR inhibitor
a novel mTOR inhibitor
1561319
1224844-38-5
Sapanisertib, 98%
Description:
a potent and selective mTOR inhibitor
a potent and selective mTOR inhibitor
1562554
1197160-78-3
Gedatolisib, 98%
Description:
a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. PKI-587 is equally effective in both complexes of mTOR, mTORC1 and mTORC2
a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. PKI-587 is equally effective in both complexes of mTOR, mTORC1 and mTORC2
1761872
914913-88-5
Palomid 529, 98%
Description:
a novel potent inhibitor of both the mTORC1 and mTORC2
a novel potent inhibitor of both the mTORC1 and mTORC2
623756
159351-69-6
Everolimus, 95%
Description:
a potent mTOR inhibitor that binds to FKBP-12 to generate an immunosuppressive complex
a potent mTOR inhibitor that binds to FKBP-12 to generate an immunosuppressive complex
628156
162635-04-3
Temsirolimus, 99%
Description:
an inhibitor of mTOR with an IC50 of 1.76 μM
an inhibitor of mTOR with an IC50 of 1.76 μM
916582
371935-74-9
PI-103, 98%
Description:
a potent PI3K/Akt and mTOR inhibitor
a potent PI3K/Akt and mTOR inhibitor
