ETC-206 is an orally available highly selective small-molecule MNK 1/2 inhibitor with IC50s of 64 nM and 86 nM, respectively.
| Molecular Weight | 408.45 |
| Formula | C25H20N4O2 |
| CAS Number | 1464151-33-4 |
| Solubility (25°C) | DMSO 82 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related MNK Products |
|---|
| EB1
EB1 is the inhibitor of kinases MNK with IC50s of 0.69 μM (MNK1) and 9.4 μM (MNK2). EB1 selectively inhibits the growth of cancer cells, but not normal cells. EB1 also increases cell apoptosis and suppresses eIF4E phosphorylation. |
| MNK inhibitor 9
MNK inhibitor 9 is a potent and selective inhibitor of MNK1/2 with IC50 values of 0.003 µM and 0.003 µM for MNK1 and MNK2 respectively. MNK inhibitor 9 has good cell permeability. MNK inhibitor 9 can be used in tumor related research. |
| WAY-305025
WAY-305025 is a selective Mnk inhibitor. |
| SLV-2436
SLV-2436 (SEL201-88) is a novel ATP-competitive inhibitor of MNK1 and MNK2 with IC50 of 10.8 nM and 5.4 nM, respectively. |
| Tomivosertib (eFT-508)
Tomivosertib (eFT-508) is a potent and selective MNK1/2 inhibitor with IC50s of 2.4 nM and 1 nM, respectively. It potentially results in decreased tumor cell proliferation and tumor growth. |
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