2. Stem Cell/Wnt
  3. β-catenin
  4. ZW4864

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 Ki 值为0.76 μM，IC50 值为 0.87 μM。

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ZW4864 Chemical Structure

ZW4864 Chemical Structure

CAS No. : 2632259-93-7

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Customer Review

Other Forms of ZW4864:

ZW4864 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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 Ki value of 0.76 μM and an IC50 value of 0.87 μM[1].

IC50 & Target

IC50: 0.87 μM (β catenin/BCL9 PPI)[1].
Ki: 0.76 μM(β catenin/BCL9 PPI)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCT-116 IC50
76 μM
Compound: 15; ZW4864
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
[PMID: 34382808]
HCT-116 IC50
76 μM
Compound: ZW4864
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured by MTS method
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured by MTS method
[PMID: 35586435]
MCF-10A IC50
92 μM
Compound: 15; ZW4864
Cytotoxicity against human MCF-10A cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
Cytotoxicity against human MCF-10A cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
[PMID: 34382808]
MCF-10A IC50
92 μM
Compound: ZW4864
Antiproliferative activity against human MCF-10A cells assessed as inhibition of cell growth measured by MTS method
Antiproliferative activity against human MCF-10A cells assessed as inhibition of cell growth measured by MTS method
[PMID: 35586435]
MDA-MB-231 IC50
28 μM
Compound: 15; ZW4864
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
[PMID: 34382808]
MDA-MB-231 IC50
28 μM
Compound: ZW4864
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured by MTS method
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured by MTS method
[PMID: 35586435]
MDA-MB-468 IC50
9.6 μM
Compound: 15; ZW4864
Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
[PMID: 34382808]
MDA-MB-468 IC50
9.6 μM
Compound: ZW4864
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth measured by MTS method
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth measured by MTS method
[PMID: 35586435]
SW480 IC50
24 μM
Compound: 15; ZW4864
Antiproliferative activity against human SW480 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
Antiproliferative activity against human SW480 cells assessed as cell growth inhibition measured after 72 hrs by MTS assay
[PMID: 34382808]
SW480 IC50
24 μM
Compound: ZW4864
Antiproliferative activity against human SW480 cells assessed as inhibition of cell growth measured by MTS method
Antiproliferative activity against human SW480 cells assessed as inhibition of cell growth measured by MTS method
[PMID: 35586435]
体外研究
(In Vitro)

ZW4864 (10~40 μM；24 hours；SW480和MBA-MD-231 cells) 降低 Axin2 和 cyclin D1 蛋白的表达水平[1]。
ZW4864 (10~40 μM；72 小时；MDA-MB231、MCF10A 和 MDA-MB-468 细胞) 选择性地触发具有过度活跃的 β-catenin 信号转导的三阴性乳腺癌细胞的快速凋亡，同时不影响正常乳腺上皮 MCF10A 细胞[1]。
ZW4864 (10~40 μM；24 小时；SW480 和 MBA-MD-231 细胞) 以浓度依赖性方式抑制 β-catenin 靶基因的转录，而不影响 HPRT 的表达，HPRT 是一种 house- Keeper 基因 (在 SW480 和 Wnt 3a 激活的 MDA-MB-231 细胞中存在)[1]。
ZW4864 剂量依赖性地抑制 β-catenin 信号激活，下调致癌 β-catenin 靶基因，并消除 β-catenin 依赖性癌细胞的侵袭力。ZW4864 以剂量依赖性方式抑制表达 β-连环蛋白的 HEK293 细胞中的 TOPFlash 荧光素酶活性，IC50 为 11 μM。ZW4864 还剂量依赖性地抑制 SW480 和 Wnt 3a 激活的 MDA-MB-468 细胞中的 TOPFlash 荧光素酶活性，IC50 分别为 7.0 和 6.3 μM。ZW4864 选择性抑制 β-catenin 信号转导的反式激活[1]。

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

ZW4864 相关抗体:

Western Blot Analysis[1]

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[1]

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[1]

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；po) 表现出良好的药代动力学特性，口服生物利用度 (F) 为 83%[1]。
ZW4864 (90 mg/kg；po) 表现出变异[1]。
ZW4864 在患者来源的异种移植小鼠模型中表现出良好的药代动力学特性并有效抑制 β-catenin 靶基因表达[1]。

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

Animal Model: C57BL/6 mice[1]
Dosage: 20 mg/kg (Pharmacokinetic Analysis)
Administration: P.o.
Result: Exhibited good pharmacokinetic properties with an oral bioavailability (F) of 83%.
Animal Model: Mice[1]
Dosage: 90 mg/kg
Administration: P.o.
Result: Showed a variation in tumor growth in mice.
分子量

607.19

Formula

C33H43ClN6O3
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 41.67 mg/mL (68.63 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

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

  • 方案 一

    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); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.43 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

    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。

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

ZW4864 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6469 mL 8.2347 mL 16.4693 mL 41.1733 mL
5 mM 0.3294 mL 1.6469 mL 3.2939 mL 8.2347 mL
10 mM 0.1647 mL 0.8235 mL 1.6469 mL 4.1173 mL
15 mM 0.1098 mL 0.5490 mL 1.0980 mL 2.7449 mL
20 mM 0.0823 mL 0.4117 mL 0.8235 mL 2.0587 mL
25 mM 0.0659 mL 0.3294 mL 0.6588 mL 1.6469 mL
30 mM 0.0549 mL 0.2745 mL 0.5490 mL 1.3724 mL
40 mM 0.0412 mL 0.2059 mL 0.4117 mL 1.0293 mL
50 mM 0.0329 mL 0.1647 mL 0.3294 mL 0.8235 mL
60 mM 0.0274 mL 0.1372 mL 0.2745 mL 0.6862 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ZW48642632259-93-7ZW 4864ZW-4864β-cateninBeta cateninorallyactiveselectiveβ cateninB-CelllymphomaproteininteractionInhibitorinhibitorinhibit

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