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
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M.Wt
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1060.66
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Formula
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C53H66ClN7O12S:
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Xin Li, et al. iScience. 2024 Jan 26;27(2):109015.
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