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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-Porcupine-RXC004
RXC004

Chemical Structure : RXC004

CAS No.: 1900754-56-4

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RXC004 (RXC-004, Zamaporvint)

货号: PC-20176Not For Human Use, Lab Use Only.

RXC004 (RXC-004, Zamaporvint) is a potent, selective Porcupine (PRCN) inhibitor, inhibits functional Wnt production from mouse L-Wnt3a cells with IC50 of 64 pM in luciferase reporters assays.

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5 mg ￥1980 In stock
10 mg ￥2980 In stock
25 mg ￥4980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

RXC004 (RXC-004, Zamaporvint) is a potent, selective Porcupine (PRCN) inhibitor, inhibits functional Wnt production from mouse L-Wnt3a cells with IC50 of 64 pM in luciferase reporters assays.
RXC004 had no effect on downstream Wnt signaling.
RXC004 inhibited palmitoylation of Wnt, RXC004 also inhibited Wnt5a secretion from L-Wnt5a cells and reduced levels of β-catenin in L-Wnt3a cells.
Porcupine inhibition by RXC004 downregulated mRNA expression of Wnt pathway targets Axin2, RNF43, c-Myc, CD44, and MMP7 in cell lines with RNF43 LoF mutations and RSPO3 fusions.
RXC004 inhibited proliferation of cell lines with RNF43 mutations and RSPO3 fusions in a concentration-dependent manner but had no effect on cell lines with mutations in downstream Wnt signaling.
RXC004 reduced the proportion of cells in S-phase, and strongly inhibited expression of the mitosis marker phospho-histone-H3 in cells with upstream aberrations in Wnt pathway components.
RXC004 treatment (5 mg/kg once daily) inhibited tumor growth in SNU-1411/NOD-SCID xenografts, with inhibition of c-Myc gene expression in tumor.

物理化学性质&存储条件

分子量 439.40
分子式 C21H16F3N7O
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

2-(5-methyl-4-(2-(trifluoromethyl)pyridin-4-yl)-1H-imidazol-1-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide

参考文献

1. Phillips C, et al. Cancer Res Commun. 2022 Sep 2;2(9):914-928.

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