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AP-1

目录号 : GC91040

一种促进ALK降解的PROTAC

AP-1 Chemical Structure

规格 价格 库存 购买数量
1 mg
¥793.00
现货
5 mg
¥3,172.00
现货
10 mg
¥5,552.00
现货

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Sample solution is provided at 25 µL, 10mM.

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AP-1 is a miniaturized proteolysis-targeting chimera (PROTAC) that contains an anaplastic lymphoma kinase (ALK) ligand connected to the E3 ubiquitin ligase ligand (±)-thalidomide by an ultrashort linker.1 It degrades the ALK fusion protein NPM-ALK in Karpas-299 cells, where it is highly expressed, when used at concentrations ranging from 10 to 300 nM, an effect that can be blocked by the proteasome inhibitor MG-132. It also degrades the ALK fusion protein EML4-ALK and ALK containing the phenylalanine-to-leucine substitution mutation at position 1174 (ALKF1174L) expressed in SN-N-SH and NCI H3122 cells, respectively. AP-1 is cytotoxic to ALK-dependent Karpas-299 cells (IC50 = 0.1265 nM) but not non-ALK-dependent THP-1 cells (IC50 = 2,704 nM). It reduces tumor volume in an NCI H3122 mouse xenograft model when administered at doses of 25, 50, and 100 mg/kg.

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1 mg 5 mg 10 mg
1 mM 1.2044 mL 6.0219 mL 12.0438 mL
5 mM 0.2409 mL 1.2044 mL 2.4088 mL
10 mM 0.1204 mL 0.6022 mL 1.2044 mL
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