P11−2 is a MNK1-Targeting PROTAC Degrader for the Treatment of Cancer. P11−2 exhibited robust antitumor activity against MV4−11cells (IC50 = 45 nM) by efficiently degrading MNK1 (DC50 = 11.92nM, Dmax > 96%) mediated by the ubiquitin-proteasome system. Notably, P11−2 does not degrade MNK2, which played an important role in maintaining normal function. Moreover, P11−2significantly suppressed the phosphorylation of eIF4E (IC50 =22.07 nM), induced apoptosis, and arrested the cell cycle at the G1phase. In addition, P11−2 exhibited favorable PK profiles and robust antitumor effects in the xenograft model.
MedKoo Cat#: 128886
Name: P11−2
CAS#: N/A
Chemical Formula: C35H38N6O6S
Exact Mass: 670.2574
Molecular Weight: 670.79
Elemental Analysis: C, 62.67; H, 5.71; N, 12.53; O, 14.31; S, 4.78
The following data is based on the product molecular weight 670.79 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 |