dEALK1 | ALK PROTAC | Probechem Biochemicals

Chemical Structure : dEALK1

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dEALK1 (ALK PROTAC)

货号: 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.

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
200 mg		Get quote
1 g		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	1060.66
分子式	C53H66ClN7O12S:
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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