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MS4077

Chemical Structure : MS4077

CAS No.: 2230077-10-6

MS4077 (MS-4077;MS 4077)

Catalog No.: PC-63529Not For Human Use, Lab Use Only.

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).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 1134.741
Formula C55H72ClN9O13S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Zhang C, et al. Eur J Med Chem. 2018 May 10;151:304-314.

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