CA-5f
目录号 : GC33218
CA-5f 是一种有效的晚期巨自噬/自噬抑制剂,通过抑制自噬体-溶酶体融合。 CA-5f 增加 LC3B-II(一种监测自噬的标志物)和 SQSTM1 蛋白,并且还增加 ROS 的产生。抗肿瘤活性。
Cas No.:1370032-19-1
Sample solution is provided at 25 µL, 10mM.
CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II (a marker to monitor autophagy) and SQSTM1 protein both in A549 cells and HUVECs. Anti-tumor activity[1].
CA-5f (0-40 μM, 6 hour) concentration- and time-dependently elevates the level of LC3B-II (a marker to monitor autophagy) and SQSTM1 protein both in A549 cells and HUVECs[1].CA-5f (20 μM, 6 hours) inhibits the degradation of autophagosomes when treated alone or in combination Bafilomycin A1 (100 nM) or Chloroquine (30 μM) in A549 cells and HUVECs[1].CA-5f (20 μM) neither impairs the hydrolytic function nor the quantity of lysosomes[1].CA-5f (20 μM, 96 hours) inhibits the growth of A549 cells, and less cytotoxic to normal HUVECs[1].|| Cell Viability Assay[1]||Cell Line:|A549, HUVECs|Concentration:|20 μM|Incubation Time:|96 hours|Result:|Exhibited more cytotoxicity against A549 cells compared with normal HUVECs.|| Western Blot Analysis[1]||Cell Line:|A549 cells and HUVECs|Concentration:|0-40 μM|Incubation Time:|6 hours|Result:|Elevated LC3B-II (a marker to monitor autophagy) and SQSTM1 protein levels in a concentration- and time-dependent manner.
CA-5f (40 mg/kg, i.p., every 2 days for up to 30 days) is well tolerated, and potently inhibits the growth of tumor in nude mice bearing A549 lung cancer cells[1]. CA-5f (40 mg/kg, i.p.) suppresses autophagic flux and induces apoptosis in nude mice bearing A549 lung cancer cells[1].|| Animal Model:|Nude mice bearing A549 lung cancer cells[1]|Dosage:|40 mg/kg|Administration:|Injected via caudal vein, every 2 days for up to 30 days|Result:|Significantly suppressed tumor volume and weight in mice, increased the number of apoptotic cells in mice.
[1]. Zhang L, et al. Identification of compound CA-5f as a novel late-stage autophagy inhibitor with potent anti-tumor effect against non-small cell lung cancer. Autophagy. 2019 Mar;15(3):391-406.
Cas No. | 1370032-19-1 | SDF | |
Canonical SMILES | O=C(/C(CN(C)C/1)=C/C2=CNC3=C2C=CC=C3)C1=C\C4=CC=C(OC)C(OC)=C4 | ||
分子式 | C24H24N2O3 | 分子量 | 388.46 |
溶解度 | DMSO : 77.5 mg/mL (199.51 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
General tips | 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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1 mg | 5 mg | 10 mg |
1 mM | 2.5743 mL | 12.8713 mL | 25.7427 mL |
5 mM | 0.5149 mL | 2.5743 mL | 5.1485 mL |
10 mM | 0.2574 mL | 1.2871 mL | 2.5743 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
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- Purity: >99.00%
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