ZX-29|cas:2254805-62-2|西域试剂

ZX-29,99.52%

产品编号：Bellancom-135887| CAS NO：2254805-62-2| 分子式：C₂₃H₂₈ClN₇O₃S| 分子量：518.03

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	价格	库存与货期
Bellancom-135887	￥3000.00	杭州北京（现货）
Bellancom-135887	￥4800.00	杭州北京（现货）
Bellancom-135887	￥9500.00	杭州北京（现货）
Bellancom-135887	￥14500.00	杭州北京（现货）

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ZX-29

产品介绍

ZX-29 是一种有效的选择性的 ALK 抑制剂，对 ALK，ALK L1196M 和 ALK G1202R 的 IC₅₀ 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。

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.

体外研究

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.
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.
ZX-29 (10 nM; 0-48 hours; NCI-H2228 cells) inhibits the proliferation of NCI-H2228 cells and arrests the cells in G1 phase.
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.
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.
ZX-29 (20 nM; 0-48 hours; NCI-H2228 cells) treatment significantly increases the mRNA level of CHOP.
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.

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

Cell Viability Assay

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

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

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

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

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

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.

西域 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
Dosage:	50 mg/kg
Administration:	Intragastric administration; every 2 days; for a total of 7 times
Result:	Showed significantly attenuated tumor growth.

体内研究

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.

西域 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
Dosage:	50 mg/kg
Administration:	Intragastric administration; every 2 days; for a total of 7 times
Result:	Showed significantly attenuated tumor growth.

体内研究

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.

西域 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
Dosage:	50 mg/kg
Administration:	Intragastric administration; every 2 days; for a total of 7 times
Result:	Showed significantly attenuated tumor growth.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (96.52 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	1.9304 mL	9.6519 mL	19.3039 mL
5 mM	0.3861 mL	1.9304 mL	3.8608 mL
10 mM	0.1930 mL	0.9652 mL	1.9304 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 (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。

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: ≥ 2.5 mg/mL (4.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.83 mM，饱和度未知) 的澄清溶液。
以 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；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