ZW4864 free base - CAS:2632259-92-6

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ZW4864 free base

目录号 : KM8903 CAS No. : 2632259-92-6 纯度 : 98%

Data Sheet 产品使用指南

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。

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5mg		In-stock
10mg		In-stock

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生物活性

ZW4864 (free base) is an orally active and selective β catenin/B-Cell lymphoma 9 protein−protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 (free base) inhibits β catenin/BCL9 PPI with a K_i value of 0.76 μM and an IC₅₀ value of 0.87 μM.

体外研究

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.

Western Blot Analysis

Cell Line:	SW480 and MBA-MD-231 cells
Concentration:	10~40 μM
Incubation Time:	24 hours
Result:	Decreased the expression levels of Axin2 and cyclin D1 proteins.

Apoptosis Analysis

Cell Line:	MDA-MB231, MCF10A and MDA-MB-468 cells
Concentration:	10~40 μM
Incubation Time:	72 hours
Result:	Selectively triggered rapid apoptosis of triple-negative breast cancer cells with hyperactive β-catenin signaling while sparing normal mammary epithelial MCF10A cells.

RT-PCR

Cell Line:	SW480 and MBA-MD-231 cells
Concentration:	10~40 μM
Incubation Time:	24 hours
Result:	Suppressed 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.

体内研究

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.

Animal Model:	C57BL/6 mice
Dosage:	20 mg/kg (Pharmacokinetic Analysis)
Administration:	P.o.
Result:	Exhibited good pharmacokinetic properties with an oral bioavailability (F) of 83%.

Animal Model:	Mice
Dosage:	90 mg/kg
Administration:	P.o.
Result:	Showed a variation in tumor growth in mice.

分子式

C₃₃H₄₂N₆O₃

分子量

570.72

CAS号

2632259-92-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度： 98%

Data Sheet

产品使用指南

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