[CAS NO. 1125593-20-5] Mps1-IN-1
PRODUCTS SPECIFICATIONS [1125593-20-5]
DESCRIPTION [1125593-20-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 535.66 |
| Molecular Formula | C28H33N5O4S |
| SMILES | O=S(C(C=CC=C1)=C1NC2=CC(NC3=C(OC)C=C(N4CCC(O)CC4)C=C3)=NC5=C2C=CN5)(C(C)C)=O |
2 Publications Citing Use of MCE
Summary
IC50 & Target
|
Mps1 367 nM (IC 50 ) |
Mps1 27 nM (Kd) |
ALK 21 nM (Kd) |
LTK 29 nM (Kd) |
PYK2 280 nM (Kd) |
FAK 440 nM (Kd) |
IGF1R 750 nM (Kd) |
|||||||
|
INSR 470 nM (Kd) |
CLK1 1900 nM (Kd) |
ERK2 2900 nM (Kd) |
INSRR 1200 nM (Kd) |
TNK1 2600 nM (Kd) |
TNK2 3100 nM (Kd) |
GAK 1100 nM (Kd) |
|||||||
In Vitro
Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC 50 and a K d of 367 nM and 27 nM. Mps1-IN-1 also has high affinity for ALK, and LTK, with K d s of 21 and 39 nM, respectively, but shows little or no inhibition on other 352 member kinases. Mps1-IN-1 (5, 10 μM) induces bypass of a checkpoint-mediated mitotic arrest in U2OS cells. Mps1-IN-1 disrupts recruitment of Mad2 to kinetochores, and reduces the phosphorylation status of Aurora B at threonine-232 (Thr232). Mps1-IN-1 (10 µM) shows no effect on centrosome duplication. In addition, Mps1-IN-1 (5-10 µM) suppresses the proliferative capacity of HCT116 [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 : ≥ 39 mg/mL ( 72.81 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.8669 mL | 9.3343 mL | 18.6686 mL |
| 5 mM | 0.3734 mL | 1.8669 mL | 3.7337 mL |
| 10 mM | 0.1867 mL | 0.9334 mL | 1.8669 mL |
-
1.