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MS4078

CAS No. : 2229036-62-6

MCE 国际站：MS4078

产品活性：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。

研究领域：PROTAC  |  Protein Tyrosine Kinase/RTK

作用靶点：PROTACs  |  Anaplastic lymphoma kinase (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：Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Heterocyclic Compound Library  |  Membrane Protein-targeted Compound Library  |  PROTAC Library  |  Highly Selective Inhibitors Library  |  LC-2  |  ACBI2  |  iRucaparib-AP6  |  BI01826025  |  ALK/ROS1-IN-1  |  BSJ-04-132  |  PROTAC VEGFR-2 degrader-1  |  SR-1114  |  Ceritinib  |  PROTAC CRABP-II Degrader-3  |  KRCA-0008  |  PROTAC Sirt2 Degrader-1  |  CRBN-6-5-5-VHL  |  PROTAC BRD2/BRD4 degrader-1  |  Iruplinalkib  |  PROTAC CDK9 degrader-8  |  BSJ-03-204  |  JPS016  |  KB02-JQ1  |  TD-802  |  BSJ-03-123  |  PROTAC RIPK degrader-6  |  ALK-IN-22  |  VZ185  |  PROTAC BRD9 Degrader-4  |  MS5033  |  PZ703b TFA  |  PROTAC FKBP Degrader-3  |  MS9449  |  SB1-G-187

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

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