| 中文名称: | ZX-29 | ||||
|---|---|---|---|---|---|
| 英文名称: | ZX-29 | ||||
| 别名: | N-(2-((5-Chloro-2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)methanesulfonamide | ||||
| CAS No: | 2254805-62-2 | 分子式: | C23H28ClN7O3S | 分子量: | 518.03 |
| CAS No: | 2254805-62-2 | ||||
| 分子式: | C23H28ClN7O3S | ||||
| 分子量: | 518.03 | ||||
包装规格：
1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介：
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。
溶解性：
溶于DMSO(50mg/ml)
储备液保存：
-80°C, 6 months
-20°C, 1 month
(protect from light)
-20°C, 1 month
(protect from light)
体内实验：
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。
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。
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。
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。
靶点：
IC50: 2.1 nM (ALK), 1.3 nM (ALK L1196M) and 3.9 nM (ALK G1202R)
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.
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.
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.
注意事项：
1、为了您的安全和健康，请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
保存条件：
2-8°C 避光
UN码：
HazardClass：
危害声明：
安全说明：
搜索质检报告(COA)
参考文献 & 客户发表文献
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
