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ZW4864 free base

CAS No. : 2632259-92-6

MCE 站：ZW4864 free base

产品活性：ZW4864 (free base) 是一种具有口服活性和选择性的 β catenin/ B-Cell lymphoma 9 蛋白-蛋白相互作用 (β catenin/BCL9 PPI) 抑制剂。ZW4864 (free base) 抑制 β catenin/BCL9 PPI 的 K_i 值为 0.76 μM，IC₅₀ 值为 0.87 μM。

研究领域：Stem Cell/Wnt

作用靶点：β-catenin

In Vitro: ZW4864 (10~40 μM; 24 hours; SW480 ａnd MBA-MD-231 cells) (free base) decreases the expression levels of Axin2 ａnd cyclin D1 proteins.
ZW4864 (10~40 μM; 72 hours; MDA-MB231, MCF10A ａnd MDA-MB-468 cells) (free base) selectively triggeres rapid apoptosis of triple-negative breast cancer cells with hyperactive β-catenin signaling while sparing normal mammary epithelial MCF10A cells.
ZW4864 (10~40 μM; 24 hours; SW480 ａnd MBA-MD-231 cells) (free base) suppresses the transcription of β-catenin target genes in a concentration-dependent manner without affecting the expression of HPRT, a house-keeper gene, in both SW480 ａnd Wnt 3a-activated MDA-MB-231 cells.
ZW4864 (free base) binds with β-catenin ａnd selectively disrupts the protein−protein interaction (PPI) between B-cell lymphoma 9 (BCL9) ａnd β-catenin while sparing the β-catenin/E-cadherin PPI. ZW4864 (free base) dose-dependently suppresses β-catenin signaling activation, downregulates oncogenic β-catenin target genes, ａnd abrogates invasiveness of β-catenin-dependent cancer cells. ZW4864 (free base) suppresses TOPFlash luciferase activities in β-catenin expressing HEK293 cells in a dose-dependent manner with an IC₅₀ of 11 μM. ZW4864 (free base) also dose-dependently suppresses the TOPFlash luciferase activities in SW480 ａnd Wnt 3a-activated MDA-MB-468 cells with the IC₅₀s of 7.0 ａnd 6.3 μM, respectively. ZW4864 (free base) selectively suppresses transactivation of β-catenin signaling.

In Vivo: ZW4864 (20 mg/kg; p.o.) (free base) exhibits good pharmacokinetic properties with an oral bioavailability (F) of 83 %.
ZW4864 (90 mg/kg; p.o.) (free base) shows a variation in tumor growth in mice.
ZW4864 (free base) shows good pharmacokinetic properties ａnd effectively suppresses β-catenin target gene expression in the patient-derived xenograft mouse model.

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