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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-ZW-49
ZW-49

Chemical Structure : ZW-49

CAS No.: 2055109-19-6

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ZW-49 (ZW49)

货号: PC-27288Not For Human Use, Lab Use Only.

ZW-49 is a potent, selective and covalent inhibitor of all subgroups of EGFR mutations with IC50 of 1.5 nM (EGFR L858R/T790M), potently inhibits all subgroups of EGFR mutations with selectivity over wild-type EGFR and other target families.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ZW-49 is a potent, selective and covalent inhibitor of all subgroups of EGFR mutations with IC50 of 1.5 nM (EGFR L858R/T790M), potently inhibits all subgroups of EGFR mutations with selectivity over wild-type EGFR and other target families.
ZW-49 shows potent anti-proliferative activity against NCI-H1975 (EGFR L858R/T790M) and HCC827 (EGFR Ex19del) with IC50 of 12 nM and 4 nM respectively, only shows moderate anti-proliferative activity for A431 (WT EGFR overexpression) cells (IC50=103 nM).
ZW-49 exhibits significant enzymatic inhibition against all tested EGFR PACC, Ex20ins, and HER2 mutants with IC50 values ranging from 0.03 to 0.41 nM.
ZW-49 shows potent cellular activity against Ba/F3 cells expressing EGFR Ex20ins (ASV, NPH, SVD, and H) mutants, and mutations G719A (PACC) and L861Q (classical-like) bearing Ba/F3 cells (IC50=0.58 and 0.98 nM).
ZW-49 blocks the G0/G1 cell cycle, triggered apoptosis, and selectively inhibits the growth of EGFR L858R/T790M mutant H1975 cells by modulating the EGFR signaling pathway.
W-49 (5 and 10 mg/kg) inhibited tumor growth in the NCI-H1975 model, ZW-49 at 25 mg/kg exhibited excellent antitumor activity with a TGI of 120.27%.

物理化学性质&存储条件

分子量 588.67
分子式 C33H32N8O3
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-(3-(2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-6-phenylpteridin-8(7H)-yl)phenyl)acrylamide

参考文献

1. Wang C, et al. Innovation (Camb). 2026 Feb 12;7(7):101313.

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