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dEALK1

Chemical Structure : dEALK1

CAS No.: 2947517-56-6

dEALK1 (ALK PROTAC)

Catalog No.: PC-21776Not For Human Use, Lab Use Only.

dEALK1 is a small-molecule degrader of EML4-ALK fusion proteins with binding constant (Kd) value of 44 nM for kinase domain of recombinant ALK, overcomes resistance to ALK inhibitor ceritinib.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

dEALK1 is a small-molecule degrader of EML4-ALK fusion proteins with binding constant (Kd) value of 44 nM for kinase domain of recombinant ALK, overcomes resistance to ALK inhibitor ceritinib.
dEALK1 is a degrader for WT and multiple ceritinib-resistant EML4-ALK mutants.
dEALK1 (100 nM) selectively degrades EML4-ALK in a CRBN-dependent manner in NSCLC cells H3122 and H2228.
dEALK1 selectively inhibits the proliferation of ALK-rearranged NSCLC cells.
dEALK1 exhibits selective antitumor activity against ALK-rearranged xenograft tumors.

Physicochemical Properties

M.Wt 1060.66
Formula C53H66ClN7O12S:
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

4-((6-(2-(2-(2-(4-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-5-isopropoxy-2-methylphenyl)piperidin-1-yl)-2-oxoethoxy)ethoxy)ethoxy)hexyl)oxy)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione

References

1. Xin Li, et al. iScience. 2024 Jan 26;27(2):109015.

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