SMK-17 is a potent MEK1/2 inhibitor with high aqueous solubility. SMK-17 inhibited MEK1 kinase activity in a non-ATP-competitive manner and it was highly selective to MEK1 and 2. SMK-17 inhibited the growth of tumor cell lines in vitro. Moreover, unlike previously reported MEK inhibitors, PD184352 or U0126, SMK-17 did not inhibit the phosphorylation of ERK5. In vivo, SMK-17 exhibited potent antitumor activity in animal models on oral administration. SMK-17 selectively blocked the MAPK pathway signaling without affecting other signal pathways, which resulted in significant antitumor efficacy without notable side effects.
MedKoo Cat#: 406623
Name: SMK-17
CAS#: 765958-29-0
Chemical Formula: C20H24ClF2IN4O2S
Exact Mass: 584.0321
Molecular Weight: 584.85
Elemental Analysis: C, 41.07; H, 4.14; Cl, 6.06; F, 6.50; I, 21.70; N, 9.58; O, 5.47; S, 5.48
The following data is based on the product molecular weight 584.85 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
