MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1, with an IC50 of 1.8 nM.
IC50&Target
Mps1
1.8 nM (IC50)
ALK
0.26 μM (IC50)
B-RAF
3.2 μM (IC50)
ERK2
3.9 μM (IC50)
FAK1
2.7 μM (IC50)
FER
0.59 μM (IC50)
FLT3
0.08 μM (IC50)
INSR
0.38 μM (IC50)
JNK1
0.11 μM (IC50)
PLK4
3.3 μM (IC50)
STK33
1.1 μM (IC50)
体外研究
MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1, with an IC50 of 1.8 nM. MPI-0479605 (0.1-10 μM) reduces cell viability of HCT-116 cells in a dose-dependent manner. MPI-0479605 shows severe defects in the ability to align chromosomes at the metaphase plate, but causes complete cytokinesis.
体内研究
MPI-0479605 (30 mg/kg daily or 150 mg/kg every fourth day (Q4D), i.p.) inhibits tumor growth by 49% and 74 % in HCT-116 xenografts. However, MPI-0479605 does not show inhibitory activity via daily dosing on the Colo-205 xenografts, and dosing every four days causes 63% tumor growth inhibition (TGI).
分子式
C22H29N7O
分子量
407.51
CAS号
1246529-32-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 11 mg/mL (26.99 mM; Need ultrasonic and warming)