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MS4078

CAS No. : 2229036-62-6

MCE 站：MS4078

产品活性：MS4078 是间变性淋巴瘤激酶 (ALK) PROTAC (降解物)，结合 ALK，K_d 为 19 nM。

研究领域：PROTAC  |  Protein Tyrosine Kinase/RTK

作用靶点：PROTAC  |  ALK

In Vitro: MS4078 effectively inhibits cancer cell proliferation. MS4078 (10^-3, 10^-2.5, 10^-2, 10^-1.5, 10^-1, 10^-0.5, 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^-2, 10^-1.5, 10^-1, 10^-0.5, 1, 10^0.5 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, MS4078 reduces the EML4-ALK protein levels with similar DC₅₀ value of?59?±?16?nM after 16-hour treatment. At the 100?nM concentration, NCI-H2228?cells reduces more than 90% of EML4-ALK protein levels.

相关产品：Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Bioactive Compound Library Plus  |  Crizotinib  |  ARV-771  |  Brigatinib  |  Lorlatinib  |  ARV-825  |  Entrectinib  |  dBET6  |  Alectinib  |  dBET1  |  Ceritinib  |  MZ 1  |  Repotrectinib  |  BETd-260  |  NVP-TAE 684  |  VH032-PEG5-C6-Cl  |  Ensartinib hydrochloride  |  A1874  |  BRD4 degrader AT1  |  BSJ-03-123  |  PROTAC K-Ras Degrader-1  |  AZD-3463  |  THAL-SNS-032  |  GSK1838705A  |  MD-224  |  PROTAC CDK9 Degrader-1  |  ALK-IN-1  |  dTRIM24

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