MNK1 PROTAC P11-2

Chemical Structure : MNK1 PROTAC P11-2

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货号: PC-24558Not For Human Use, Lab Use Only.

MNK1 PROTAC P11-2 is a first-in-class, selective MNK1-targeting PROTAC degrader with DC50 of 11.92 nM (MV4-11 cells), Dmax>96%, shows remarkable selectivity for MNK1 over MNK2.

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100 mg		Get quote

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生物&药学活性

MNK1 PROTAC P11-2 is a first-in-class, selective MNK1-targeting PROTAC degrader with DC50 of 11.92 nM (MV4-11 cells), Dmax>96%, shows remarkable selectivity for MNK1 over MNK2.
P11-2 rapidly degraded MNK1 at the dose of 300 nM, with a t1/2 value of 3.64 h.
P11-2 exhibited MNK1 degradation activity in other cancer cell lines, including MOLM-13, MM.1S, and MDA-MB-231.
P11-2 significantly decreased both MNK1 and p-eIF4E levels (IC50 = 22.07 nM), demonstrating superior efficacy compared to DS12881479.
P11-2 induced apoptosis, and arrested the cell cycle at the G1 phase.
P11-2 (20 mg/kg) exhibited favorable PK profiles and robust antitumor effects in xenograft mouse model by subcutaneously transplanting MV4–11 cells.

物理化学性质&存储条件

分子量	670.79
分子式	C35H38N6O6S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-(7-((2-(2,6-Dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)amino)-7-oxoheptanoyl)-N-(5-phenylthiazol-2-yl)piperidine-4-carboxamide

参考文献

1. Yang Z, et al. J Med Chem. 2025 May 7. doi: 10.1021/acs.jmedchem.5c00062.

MNK1 PROTAC P11-2

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