[CAS NO. 1246529-32-7] MPI-0479605
PRODUCTS SPECIFICATIONS [1246529-32-7]
DESCRIPTION [1246529-32-7]
Overview
| MDL | MFCD28099811 |
|---|---|
| Molecular Weight | 407.51 |
| Molecular Formula | C22H29N7O |
| SMILES | CC(C=C(N1CCOCC1)C=C2)=C2NC3=NC4=C(N=CN4)C(NC5CCCCC5)=N3 |
2 Publications Citing Use of MCE
Summary
MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1 , with an IC 50 of 1.8 nM.
IC50 & Target
|
Mps1 1.8 nM (IC 50 ) |
ALK 0.26 μM (IC 50 ) |
B-RAF 3.2 μM (IC 50 ) |
ERK2 3.9 μM (IC 50 ) |
FAK1 2.7 μM (IC 50 ) |
FER 0.59 μM (IC 50 ) |
FLT3 0.08 μM (IC 50 ) |
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|
INSR 0.38 μM (IC 50 ) |
JNK1 0.11 μM (IC 50 ) |
PLK4 3.3 μM (IC 50 ) |
STK33 1.1 μM (IC 50 ) |
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In Vitro
MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1, with an IC 50 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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 11 mg/mL ( 26.99 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4539 mL | 12.2696 mL | 24.5393 mL |
| 5 mM | 0.4908 mL | 2.4539 mL | 4.9079 mL |
| 10 mM | 0.2454 mL | 1.2270 mL | 2.4539 mL |