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首页-抗体药物偶连体和PROTACs-PROTAC-WZH-17-002
WZH-17-002

Chemical Structure : WZH-17-002

CAS No.:

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WZH-17-002

货号: PC-24804Not For Human Use, Lab Use Only.

WZH-17-002 is a potent, selective ALK PROTAC degrader with DC50 of 25 nM both in H3122 and DFCI076 cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

WZH-17-002 is a potent, selective ALK PROTAC degrader with DC50 of 25 nM both in H3122 and DFCI076 cells.
WZH-17-002 exhibits anti-proliferative activitiy with IC50 of 17.2 and 15.0 nM against EML4-ALK-G1202R/L1196M and EML4-ALK-L1196M/D1203N Ba/F3 cells respectively.
WZH-17-002 selectively inhibits three NSCLC with ALK rearrangements, DFCI076, H3122 and H2228, with IC50 values of 8.6 nM, 4.5 nM and 58.6 nM, respectively.
WZH-17-002 also exhibits moderate activity against EGFR-driven NSCLC such as PC9 with an IC50 of 179.4 nM.
WZH-17-002 effectively reduces ALK protein levels in H2228 cells with ALK-rearrangement at a low dose of 5 nM, WZH-17-002 also markedly reduces the total ALK protein and phosphorylation levels in Ba/F3 cells expressing EML4-ALK compound mutations such as G1202R/L1196M and I1171S/G1269A.
WZH-17-002 degrades ALK through the proteasome mediated pathway.
WZH-17-002 suppresses the emergence of drug resistance in ALK-fusion NSCLC.
WZH-17-002 (10 mpk or 20 mpk, i.v. injection) exhibits in vivo efficacy in EML4-ALK G1202R/L1196 M Ba/F3 xenograft mouse models.

物理化学性质&存储条件

分子量 1044.98
分子式 C47H54BrN11O10S
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

N-(6-((5-bromo-2-((4-(4-(4-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)glycyl)piperazin-1-yl)piperidin-1-yl)-5-ethyl-2-methoxyphenyl)amino)pyrimidin-4-yl)amino)-2,3-dihydrobenzo[b][1,4]dioxin-5-yl)-N-methylmethanesulfonamide

参考文献

1. Gao F, et al. Eur J Med Chem. 2025 Jun 2;296:117835.

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