计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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 IC 50 value of 0.87 μM
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 IC 50 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 IC 50 s of 7.0 and 6.3 μM, respectively. ZW4864 (free base) selectively suppresses transactivation of β-catenin signaling. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell 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 AnalysisCell 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-PCRCell 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.
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.
IC50& Target:IC50: 0.87 μM (β catenin/BCL9 PPI),Ki: 0.76 μM (β catenin/BCL9 PPI)
规格
别名
ZW4864 游离碱
规格或纯度
10mM in DMSO
英文名称
ZW4864 free base
生化机理
ZW4864（游离碱）是一种具有口服活性和选择性的 β 连环素/细胞淋巴瘤 9 蛋白-蛋白相互作用（β 连环素/BCL9 PPI）抑制剂。ZW4864 （游离碱基）抑制 β 连环素/BCL9 PPI 的 K i 值为 0.76 μM，IC 50 值为 0.87 μM。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
分子量
570.72
技术文档
高级数据
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 2632259-92-6，分子式为 C33H42N6O3，分子量为 570.72 g/mol。
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