ZW4864|cas:2632259-93-7|西域试剂

ZW4864,97.08%

产品编号：Bellancom-132300| CAS NO：2632259-93-7| 分子式：C₃₃H₄₃ClN₆O₃| 分子量：607.19

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	包装	价格	库存与货期	购买量	操作
Bellancom-132300		￥5000.00	杭州北京（现货）
Bellancom-132300		￥8500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

ZW4864

产品介绍

ZW4864 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 抑制 β catenin/BCL9 PPI 的 K_i 值为0.76 μM，IC₅₀ 值为 0.87 μM。

生物活性

ZW4864 is an orally active and selective β catenin/B-Cell lymphoma 9 protein−protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 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) decreases the expression levels of Axin2 and cyclin D1 proteins.
ZW4864 (10~40 μM; 72 hours; MDA-MB231, MCF10A and MDA-MB-468 cells) 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) 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 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 dose-dependently suppresses β-catenin signaling activation, downregulates oncogenic β-catenin target genes, and abrogates invasiveness of β-catenin-dependent cancer cells. ZW4864 suppresses TOPFlash luciferase activities in β-catenin expressing HEK293 cells in a dose-dependent manner with an IC₅₀ of 11 μM. ZW4864 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 selectively suppresses transactivation of β-catenin signaling.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(In Vivo)

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

西域 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.

体内研究

西域 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.

体内研究

西域 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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 41.67 mg/mL (68.63 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6469 mL	8.2347 mL	16.4693 mL
5 mM	0.3294 mL	1.6469 mL	3.2939 mL
10 mM	0.1647 mL	0.8235 mL	1.6469 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.43 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.43 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.43 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.43 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。