MS4078 是基于 Cereblon 配体的间变性淋巴瘤激酶 (ALK) PROTAC (降解物)，结合 ALK，K_d 为 19 nM。

MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a K d of 19?nM for binding affinity to ALK.

Solid

ALK Cereblon

MS4078 effectively inhibits cancer cell proliferation. MS4078 (10, 10, 10, 10, 10, 10, 1 μM; 3 days) concentration-dependently inhibits proliferation of SU-DHL-1?cells with an IC50?of?33±1??nM. In comparison with SU-DHL-1?cells, the proliferation of NCI-H2228?cells is less sensitive to MS4078(10, 10, 10, 10, 1, 10 μM; 3 days).
MS4078 potently reduces the ALK fusion protein levels and inhibits the ALK auto-phosphorylation and down-steam STAT3 phosphorylation in both SU-DHL-1 and NCI-H2228?cells in a concentration-dependent manner. In SU-DHL-1?cells, MS4078 reduces the NPM-ALK protein levels with impressive DC50 (50% degradation) value of?11±2?nM after 16-hour treatment. Over 90% of inhibition of both ALK Y1507 and STAT3 Y705 phosphorylation is achieved at the 100?nM concentration. In NCI-H2228?cells

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Zhang C, et al. Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK). Eur J Med Chem. 2018 May 10;151:304-314.

In Vitro: DMSO : 50 mg/mL (54.68 mM; Need ultrasonic)配制储备液