Chemical Structure : WNTinib
CAS No.: 2770091-44-4
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.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥1280 | In stock | |
10 mg | ¥1980 | In stock | |
25 mg | ¥3580 | In stock | |
50 mg | ¥5580 | In stock | |
100 mg | Get quote |
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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.
分子量 | 498.39 | |
分子式 | C22H16F6N4O3 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
4-(3-fluoro-4-(3-(4-(perfluoroethyl)phenyl)ureido)phenoxy)-N-methylpicolinamide |
1. Rialdi A, et al. Nat Cancer. 2023 Aug 3. doi: 10.1038/s43018-023-00609-9.
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