MS4077

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MS4077 是一种新型的 ALK PROTAC（降解剂），在 SU-DHL-1 淋巴瘤和 NCI-H2228 肺癌细胞中以浓度和时间依赖性方式有效降低致癌活性 ALK 融合蛋白的细胞水平 (DC50=3 nM) 。

MS4077 is a novel PROTAC (degrader) of ALK, potently decreases cellular levels of oncogenic active ALK fusion proteins in a concentration- and time-dependent manner in SU-DHL-1 lymphoma and NCI-H2228 lung cancer cells (DC50=3 nM); induces ALK protein degradation via cereblon and proteasome dependent mechanism, potently inhibits proliferation of SU-DHL-1?cells with IC50 of 46 nM.

Cell Viability Assay Cell Line:SU-DHL-1 and NCI-H2228 cellsConcentration:10-3, 10-2.5, 10-2,10-1.5, 10-1, 10-0.5, and 1 μM for SU-DHL-1 ?cells; 10-2, 10-1.5, 10-1, 10-0.5, 1, 100.5 μM for NCI-H2228?cells Incubation Time:3 days Result:Inhibited proliferation of SU-DHL-1?cells (IC50=46?±?4?nM). Less sensitive to the proliferation of NCI-H2228?cells than SU-DHL-1?cells.Western Blot Analysis Cell Line:SU-DHL-1 and NCI-H2228 cells Concentration:1, 3, 10, 30, and 100 μM for SU-DHL-1 cells; 3, 10, 30, 60, and 100 μM for NCI-H2228 cells Incubation Time:16?hours Result:Reduced the NPM-ALK protein levels with impressive DC50 of ?3?±?1?nM in SU-DHL-1?cells. Reduced the EML4-ALK protein levels with similar DC50 of?34?±?9?nM in NCI-H2228?cells.

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MS-4077 | MS 4077

PROTACs

PROTAC

PROTAC

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2230077-10-6

1134.741

C55H72ClN9O13S

>98% (HPLC)

In Vitro:?DMSO : 110 mg/mL (96.94 mM)

CC1=CC(=C(C=C1C2CCN(CC2)CC(=O)NCCOCCOCCOCCOCCOCCNC3=CC=CC4=C3C(=O)N(C4=O)C5CCC(=O)NC5=O)OC(C)C)NC6=NC=C(C(=N6)NC7=CC=CC=C7S(=O)(=O)C(C)C)Cl

2-(4-(4-((5-Chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-5-isopropoxy-2-methylphenyl)piperidin-1-yl)-N-(17-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-3,6,9,12,15-pentaoxaheptadecyl)acetamide

(-20℃)

With Ice Pack

≥ 2 years