1. Protein Tyrosine Kinase/RTK Apoptosis Autophagy
  2. Anaplastic lymphoma kinase (ALK) Apoptosis Autophagy
  3. ZX-29

ZX-29 是一种有效的选择性的 ALK 抑制剂,对 ALKALK L1196MALK G1202RIC50 分别为 2.1 nM,1.3 nM 和 3.9 nM,但对 EGFR 无活性。ZX-29 通过诱导内质网应激来诱导细胞凋亡 (apoptosis),并克服了由 ALK 突变引起的细胞抗性。ZX-29 还可诱导保护性自噬 (autophagy) 并具有抗肿瘤作用。

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ZX-29 Chemical Structure

ZX-29 Chemical Structure

CAS No. : 2254805-62-2

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect[1].

IC50 & Target

IC50: 2.1 nM (ALK), 1.3 nM (ALK L1196M) and 3.9 nM (ALK G1202R)[1]

体外研究
(In Vitro)

ZX-29 (0-81 nM; 24-72 hours; NCI-H2228 cells) treatment leads to a time- and dose-dependent decrease in NCI-H2228 cell viability[1].
ZX-29 (10 nM; 24 hours; NCI-H2228 cells) treatment causes typical signs of autophagy and the formation of autophagosomes. ZX-29 enhances the expression level of LC3 and Beclin1[1].
ZX-29 (10 nM; 0-48 hours; NCI-H2228 cells) inhibits the proliferation of NCI-H2228 cells and arrests the cells in G1 phase[1].
ZX-29 (10-40 nM; 24-48 hours; NCI-H2228 cells) treatment induces apoptosis of NCI-H2228 cells. ZX-29 dose-dependently upregulates the expression levels of proapoptotic protein Bax, increases the production of activated forms of caspase 3, and downregulates the expression level of antiapoptotic protein Bcl-2[1].
ZX-29 (30-300 nM; 24 hours; NCI-H2228 cells) treatment significantly down-regulates the expression of p-ALK and its downstream signaling proteins, including p-Akt and p-STAT3, in a dose-dependent manner[1].
ZX-29 (20 nM; 0-48 hours; NCI-H2228 cells) treatment significantly increases the mRNA level of CHOP[1].
ZX-29 dose-dependently inhibits colony formation of NCI-H2228 cells. With an increase in ZX-29 concentration, the cell density decreased gradually, and the cells lost their normal morphology and become sharp and slender[1].

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

Cell Viability Assay[1]

Cell Line: NCI-H2228 cells
Concentration: 0 nM, 1 nM, 3 nM, 9 nM, 10 nM, 27 nM or 81 nM
Incubation Time: 24 hours, 48 hours or 72 hours
Result: Led to a time- and dose-dependent decrease in NCI-H2228 cell viability.

Cell Autophagy Assay[1]

Cell Line: NCI-H2228 cells
Concentration: 10 nM
Incubation Time: 24 hours
Result: Caused typical signs of autophagy and the formation of autophagosomes.

Cell Cycle Analysis[1]

Cell Line: NCI-H2228 cells
Concentration: 0 hour, 12 hours, 24 hours or 48 hours
Incubation Time: 24 hours
Result: Arrested the NCI-H2228 cells in G1 phase in a time-dependent manner.

Apoptosis Analysis[1]

Cell Line: NCI-H2228 cells
Concentration: 10 nM, 20 nM or 40 nM
Incubation Time: 24 hours, 48 hours
Result: Promoted NCI-H2228 cell apoptosis in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: NCI-H2228 cells
Concentration: 30 nM, 100 nM, 300 nM
Incubation Time: 24 hours
Result: Significantly down-regulated the expression of p-ALK and its downstream signaling proteins, including p-Akt and p-STAT3, in a dose-dependent manner.

RT-PCR[1]

Cell Line: NCI-H2228 cells
Concentration: 20 nM
Incubation Time: 0 hour, 6 hours, 12 hours, 24 hours or 48 hours
Result: The mRNA level of CHOP was increased significantly.
体内研究
(In Vivo)

ZX-29 (50 mg/kg; intragastric administration; every 2 days; for a total of 7 times; female BALB/c nude mice) treatment suppresses tumor growth in a mouse xenograft model[1].

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

Animal Model: Female BALB/c nude mice (4-week-old) with H2228 cells[1]
Dosage: 50 mg/kg
Administration: Intragastric administration; every 2 days; for a total of 7 times
Result: Showed significantly attenuated tumor growth.
分子量

518.03

Formula

C23H28ClN7O3S

CAS 号
性状

固体

颜色

Light yellow to green yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 50 mg/mL (96.52 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 1.9304 mL 9.6519 mL 19.3039 mL
5 mM 0.3861 mL 1.9304 mL 3.8608 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 (protect from light)。-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

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

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.83 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 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。
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

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 (protect from light)

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

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 (protect from light)。-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 1.9304 mL 9.6520 mL 19.3039 mL 48.2598 mL
5 mM 0.3861 mL 1.9304 mL 3.8608 mL 9.6520 mL
10 mM 0.1930 mL 0.9652 mL 1.9304 mL 4.8260 mL
15 mM 0.1287 mL 0.6435 mL 1.2869 mL 3.2173 mL
20 mM 0.0965 mL 0.4826 mL 0.9652 mL 2.4130 mL
25 mM 0.0772 mL 0.3861 mL 0.7722 mL 1.9304 mL
30 mM 0.0643 mL 0.3217 mL 0.6435 mL 1.6087 mL
40 mM 0.0483 mL 0.2413 mL 0.4826 mL 1.2065 mL
50 mM 0.0386 mL 0.1930 mL 0.3861 mL 0.9652 mL
60 mM 0.0322 mL 0.1609 mL 0.3217 mL 0.8043 mL
80 mM 0.0241 mL 0.1206 mL 0.2413 mL 0.6032 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.

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HY-135887
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