MS4078 是一种基于 Cereblon 配体的间变性淋巴瘤激酶 PROTAC ，结合 ALK 的 Kd为 19 nM。

MS4078 is an inhibitor and aplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19 nM for binding affinity to ALK.

MS4078 effectively inhibits cancer cell proliferation. MS4078 induces ALK protein degradation via cereblon and proteasome dependent mechanism and potently inhibits proliferation of SU-DHL-1?cells with IC50 of 33 nM. 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. MS4078 reduces the NPM-ALK protein levels in SU-DHL-1 cells and the EML4-ALK protein levels in NCI-H2228 cells with DC50 of 11 nM and 59 nM, respectively.

2229036-62-6

C45H52ClN9O8S

914.47

DMSO:49 mg/mL (53.58 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years