MS4077

MS4077 is an ALK PROTAC degrader with a DC₅₀ of 3 nM in SU-DHL-1 cells, a DC₅₀ of 34 nM in NCI-H2228 cells, and a K_d of 37 nM. MS4077 induces the degradation of oncogenic active ALK fusion proteins via a cereblon- and proteasome-dependent pathway, and inhibits the phosphorylation of ALK and STAT3, thereby suppressing cancer cell proliferation. MS4077 is used for the research of anaplastic large cell lymphoma and non-small cell lung cancer^[1][2][3][4]. IC50 & Target:Kd: 37±4nM (ALK)^[1]
PROTAC^[1] In Vitro:MS4077 degrades NPM-ALK and EML4-ALK, inhibits the phosphorylation of ALK and STAT3 in a concentration- and time-dependent manner, and exhibits potent antiproliferative activity in SU-DHL-1 ALCL cells^[4].
MS4077 (1-100 nM; 2-24 h) degrades the NPM-ALK protein in SU-DHL-1 cells in a concentration- and time-dependent manner, with a DC₅₀ of 3 nM. It inhibits the phosphorylation of downstream ALK and STAT3 via cereblon-dependent and proteasome-dependent mechanisms, and these effects are reversible after washout of the compound^[1].
MS4077 (3-100 nM; 2-24 h) degrades the EML4-ALK protein in NCI-H2228 cells in a concentration- and time-dependent manner, with a DC₅₀ of 34 nM, and inhibits the downstream phosphorylation of ALK^[1].
MS4077 (3 days) potently inhibits the proliferation of SU-DHL-1 cells, with an IC₅₀ of 46 nM^[1].
MS4077 (compound 5) binds to purified ALK protein with high affinity, with a K_d value of 37 nM^[1].
MS4077 potently downregulates the protein levels of ALK and PFKFB3 in the anaplastic large cell lymphoma cell line SU-DHL-1^[2].