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MS4077

CAS No. : 2230077-10-6

MCE 站：MS4077

产品活性：MS4077 是间变性淋巴瘤激酶 (ALK) PROTAC (降解物)，结合 ALK, K_d 为 37 nM。

研究领域：PROTAC  |  Protein Tyrosine Kinase/RTK

作用靶点：PROTAC  |  ALK

In Vitro: MS4077 effectively inhibits cancer cell proliferation. MS4077 (10^-3-1 μM; 3 days) concentration-dependently inhibits proliferation of SU-DHL-1?cells with an IC₅₀?of?46?±?4?nM. In comparison with SU-DHL-1?cells, the proliferation of NCI-H2228?cells is less sensitive to MS4077(10^-2-10^0.5 μM; 3 days).
MS4077 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, MS4077 reduces the NPM-ALK protein levels with impressive DC₅₀ (50% degradation) value of?3±1?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, MS4077 reduces the EML4-ALK protein levels with similar DC₅₀ value of?34±9?nM after 16-hour treatment. At the 100?nM concentration, NCI-H2228?cells reduces more than 90% of EML4-ALK protein levels.

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