LYN-1604
目录号 : GC19236
A ULK1 activator
Cas No.:2088939-99-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Kinase experiment: |
Cells or tumor tissues are treated with LYN-1604 for the indicated times. Both adherent and floating cells are collected and western blot analysis is carried out. Briefly, the cell pellets ae resuspended with lysis buffer consisting of 50 mM HEPES, pH 7.4; 1% Triton-X-100, 2 mM sodium orthovanadate, 100 mM sodium fluoride, 1 mM edetic acid, 1 mM PMSF, 10 mg/L aprotinin and 10 mg/Lleupeptin, and lysed at 4°C for 1 h. After 12?000 rpm centrifugation for 15 min, the protein content of the supernatant is determined by the Bio-Rad DC protein assay[1]. |
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Cell experiment: |
Cells are dispensed in 96-well plates at a density of 5×104 cells per mL. After 24 h of incubation, cells are treated with different concentrations of LYN-1604 for the indicated time periods. Cell viability is measured by the MTT assay[1]. |
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Animal experiment: |
24 female nude mice (BALB/c, 6 to 8 weeks, 20 to 22 g) are used and injected subcutaneously with MDA-MB-231 cells (5×106 cells per mouse). When the tumors reach 100 mm3 in volume (V=L×W2/2), the mice are divided into four groups. Three groups are treated with different doses of LYN-1604 once a day by intragastric administration for 14 days (low dose, 25 mg/kg; median dose, 50 mg/kg; high dose, 100 mg/kg), whereas the control group is treated with vehicle control. During the treatment, the tumor volumes and body weight are measured every day until the end of the study. At the end of treatment, all mice are sacrificed. The spleen, liver, kidney and tumor tissue are harvested, weighed, and photographed, then immediately frozen in liquid nitrogen or fixed in formalin[1]. |
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References: [1]. Zhang L, et al. Discovery of a small molecule targeting ULK1-modulated cell death of triple negative breast cancer in vitro and in vivo. Chem Sci. 2017 Apr 1;8(4):2687-2701. |
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LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) agonist with an EC50 of 18.94 nM.
LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) agonist with an EC50 of 18.94 nM in ADP-Glo™ kinase assay. The in vitro kinase assay reveals that the LYN-1604 increases the phosphorylation of mATG13 at ser318 in wild-type ULK1 transfected HEK-293T cells. It is found that LYN-1604-treated cells display a remarkable green fluorescence with MDC staining and the autophagy ratio is increased in a dose-dependent manne. It is also found that LYN-1604 induces remarkable up-regulation of Beclin-1 and degradation of p62, as well as transformation of LC3-I to LC3-II[1].
Based on the results of tumor volume and weight, it is found that LYN-1604 can significantly inhibit the growth of xenograft MDA-MB-231 cells. The body weights of mice are stable, with no obvious distinctions between LYN-1604-treated and control mice. It also reveals that LYN-1604 induces remarkable autophagy in vivo[1].
References:
[1]. Zhang L, et al. Discovery of a small molecule targeting ULK1-modulated cell death of triple negative breast cancer in vitro and in vivo. Chem Sci. 2017 Apr 1;8(4):2687-2701.
| Cas No. | 2088939-99-3 | SDF | |
| Canonical SMILES | ClC1=CC=C(C(CN2CCN(C(CN(CC(C)C)CC(C)C)=O)CC2)OCC3=CC=C(C=CC=C4)C4=C3)C(Cl)=C1 | ||
| 分子式 | C33H43Cl2N3O2 | 分子量 | 584.62 |
| 溶解度 | DMSO : 100 mg/mL (161.01 mM) | 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 | 1.7105 mL | 8.5526 mL | 17.1051 mL |
| 5 mM | 0.3421 mL | 1.7105 mL | 3.421 mL |
| 10 mM | 0.1711 mL | 0.8553 mL | 1.7105 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。