供应商:
Kinasechem
CAS号:
1032350-13-2
保存条件:
-20° C
保质期:
2 年
数量:
大量
规格:
2mg/5mg/10mg
规格: |
|
产品价格: |
¥900 |
规格: |
2mg |
产品价格: |
¥900 |
规格: |
5mg |
产品价格: |
¥1200 |
规格: |
10mg |
产品价格: |
¥1700 |
MK-2206 can inhibit Akt1, Akt2, and Akt3 with IC50 of 8 nM, 12 nM, and 65 nM. As a novel allosteric Akt inhibitor, MK-2206 can synergistically inhibited cell proliferation of human cancer cell lines. MK-2206 causes growth inhibition of the eight cell lines with an IC50 that ranges between 3.4 and 28.6 μmol/L. MK-2206 alone more potently inhibited the cell growth of Ras wild-type (WT) cell lines (A431, HCC827, and NCI-H292; IC50 s of 5.5, 4.3, and 5.2 μmol/L, respectively) as compared with Ras-mutant cell lines (NCI-H358, NCI-H23, NCI-H1299, and Calu-6; IC50 s of 13.5, 14.1, 27.0, and 28.6 μmol/L, respectively), with the exception of NCI-H460, which has a PIK3CA E545K mutation (IC50 , 3.4 μmol/L).In acute lymphoblastic leukemia, MK-2206 decreased T-ALL cell line viability by blocking leukemic cells in the G(0)/G(1) phase of the cell cycle and inducing apoptosis. MK-2206 also induced autophagy. In acute lymphoblastic leukemia, MK-2206 lead to a concentration-dependent dephosphorylation of Akt and its downstream targets, GSK-3alpha/beta and FOXO3A. In Neuroblastoma, MK-2206 treatment inhibited NB cell proliferation which was accompanied by a cell line selective G1 arrest of cell cycle or production of ROS.
温馨提示:不可用于临床ZL。