ERK1/2 inhibitor 2 (Example 1) is a potent dual ERK1/2 inhibitor. ERK1/2 inhibitor 2 has anti-cancer activity.
| Molecular Weight | 584.04 |
| Formula | C29H31ClFN5O5 |
| CAS Number | 2095719-92-7 |
| Solubility (25°C) | DMSO ≥ 60 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.
[5] Robert Roskoski Jr. Pharmacol Res. ERK1/2 MAP kinases: structure, function, and regulation
| Related ERK Products |
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| PACAP-38 (31-38), human, mouse, rat
PACAP-38 (31-38), human, mouse, rat is a PAC1 receptor activator and increases the α-secretase activity. |
| Endothelin-1 (1-31) (Human)
Endothelin-1 (1-31) (Human) is a potent vasoconstrictor and hypertensive agent. |
| ZINC12409120
ZINC12409120 is a high selective ERK inhibitor. |
| Tizaterkib (hexanedioic acid)
Tizaterkib hexanedioic acid is a potent and selective ERK2 inhibitor, with an IC50 of 0.6 nM. |
| TAT-MEK1
TAT-MEK1 is an inhibitor ofERK2, consisting of TAT and MEK1 (N-terminal), TAT (YGRKKRRQRRR) derived from human immunodeficiency (HIV-1) transcriptional trans activator (TAT), is a cell-penetrating peptide. |
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