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WNTinib

Chemical Structure : WNTinib

CAS No.: 2770091-44-4

WNTinib (APS-8-100-2)

货号: PC-20893Not For Human Use, Lab Use Only.

WNTinib is a multi-kinase inhibitor with specificity against β-catenin (CTNNB1) mutant hepatocellular carcinoma, harnesses the KIT/MAPK/EZH2 pathway, shows durable and selective transcriptional repression of mutant β-catenin/Wnt targets through nuclear translocation of the EZH2 transcriptional repressor.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

WNTinib (APS-8-100-2) is a multi-kinase inhibitor with specificity against β-catenin (CTNNB1) mutant hepatocellular carcinoma, harnesses the KIT/MAPK/EZH2 pathway, shows durable and selective transcriptional repression of mutant β-catenin/Wnt targets through nuclear translocation of the EZH2 transcriptional repressor.
WNTinib reduces EZH2 phosphorylation to drive the suppression of essential gene networks in CTNNB1-mutated HCC.
WNTinib depends on EZH2 relocalization to chromatin for its activity in CTNNB1-mutated HCC.
WNTinib utilizes unique polypharmacology to regulate the EZH2–WNT axis.
KIT, BRAF and p38 kinases are critical anti-targets for WNTinib.
WNTinib outperforms clinical compounds across in vivo models of HCC.

物理化学性质&存储条件

分子量 498.39
分子式 C22H16F6N4O3
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-(3-fluoro-4-(3-(4-(perfluoroethyl)phenyl)ureido)phenoxy)-N-methylpicolinamide

参考文献

1. Rialdi A, et al. Nat Cancer. 2023 Aug 3. doi: 10.1038/s43018-023-00609-9.

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