LYG-202
目录号 : GC40865
LYG-202是一种具有哌嗪取代基的合成黄酮类化合物，展现出显著的抗肿瘤活性。
Cas No.:1175077-25-4
Sample solution is provided at 25 µL, 10mM.
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LYG-202 is a synthesized flavonoid with a piperazine substitution, exhibiting potent antitumor effects[1]. LYG-202 has been widely used to inhibit angiogenesis in different xenograft tumor mouse models[2].
In vitro, LYG-202 treatment for 24h inhibited the viabilities of HepG2, MCF-7, HeLa, BGC-823, MDA-MB-435, and HCT-116 cells, with the IC50 values of 4.74±0.80, 27.70±1.09, 8.05±0.21, 6.42±1.40, 6.74±0.71, and 10.90±0.95μM, respectively[3]. Pretreatment of J774A.1 cells with 4µM LYG-202 for 1 hour improved the thermostability of ALDOA enzyme and inhibited ALDOA hydrolysis[4]. Treatment of HepG2 cells with 8µM LYG-202 for 24h resulted in a decrease in mitochondrial membrane potential and intracellular ATP and increased intracellular ROS levels[5]. Treatment with 10µM LYG-202 for 8 hours inhibited vascular endothelial growth factor (VEGF)-stimulated human umbilical vein endothelial cell (HUEVC) migration and tube formation[6].
In vivo, LYG-202 treatment via intravenous injection at a dose of 20mg/kg/2-day for 3 weeks inhibited tumor growth in xenograft mice bearing MCF-7 tumor[7]. Along with the subcutaneous injection of TNF-α (1.5µg/day), LYG-202 treatment (p.o) inhibited H22 solid tumor growth in a xenograft mouse model at a dose of 750mg/kg every two days for 7 days[8].
References:
[1] Al-Ghorbani M, Gouda M A, Baashen M, et al. Piperazine heterocycles as potential anticancer agents: A review[J]. Pharmaceutical Chemistry Journal, 2022, 56(1): 29-37.
[2] Zhao K, Yao Y, Luo X, et al. LYG-202 inhibits activation of endothelial cells and angiogenesis through CXCL12/CXCR7 pathway in breast cancer[J]. Carcinogenesis, 2018, 39(4): 588-600.
[3] Zeng S, Liu W, Nie F, et al. LYG-202, a new flavonoid with a piperazine substitution, shows antitumor effects in vivo and in vitro[J]. Biochemical and biophysical research communications, 2009, 385(4): 551-556.
[4] Bai D, Du J, Bu X, et al. ALDOA maintains NLRP3 inflammasome activation by controlling AMPK activation[J]. Autophagy, 2022, 18(7): 1673-1693.
[5] Chen F, Zhang L, Qiang L, et al. Reactive oxygen species-mitochondria pathway involved in LYG-202-induced apoptosis in human hepatocellular carcinoma HepG2 cells[J]. Cancer Letters, 2010, 296(1): 96-105.
[6] Chen Y, Lu N, Ling Y, et al. LYG-202, a newly synthesized flavonoid, exhibits potent anti-angiogenic activity in vitro and in vivo[J]. Journal of pharmacological sciences, 2010, 112(1): 37-45.
[7] Zhao Y, Wang X, Sun Y, et al. LYG-202 exerts antitumor effect on PI3K/Akt signaling pathway in human breast cancer cells[J]. Apoptosis, 2015, 20(9): 1253-1269.
[8] Chen F, Lu N, Zhang H, et al. LYG-202 augments tumor necrosis Factor-α-Induced apoptosis via attenuating casein kinase 2-Dependent nuclear Factor-κB pathway in HepG2 cells[J]. Molecular pharmacology, 2012, 82(5): 958-971.
LYG-202是一种具有哌嗪取代基的合成黄酮类化合物，展现出显著的抗肿瘤活性[1]。该化合物已在多种移植瘤小鼠模型中广泛应用于抑制血管生成[2]。
在体外，LYG-202处理24小时可抑制HepG2、MCF-7、HeLa、BGC-823、MDA-MB-435和HCT-116细胞的活力，IC50值分别为4.74±0.80、27.70±1.09、8.05±0.21、6.42±1.40、6.74±0.71和10.90±0.95μM[3]。用4μM的LYG-202预处理J774A.1细胞1小时，能提高ALDOA酶的热稳定性并抑制酶水解[4]。使用8μM的LYG-202处理HepG2细胞24小时，可导致线粒体膜电位和细胞内ATP水平下降，同时增加活性氧含量[5]。以10μM的LYG-202处理人脐静脉内皮细胞(HUEVC)8小时，能抑制血管内皮生长因子(VEGF)刺激的细胞迁移和管状结构形成[6]。
在体内，每两天静脉注射20mg/kg剂量的LYG-202持续3周，可抑制MCF-7移植瘤小鼠的肿瘤生长[7]。在每日皮下注射TNF-α的条件下，每两天口服750mg/kg剂量的LYG-202连续7天，能抑制H22实体瘤移植瘤模型的肿瘤生长[8]。
| Cell experiment [1]: | |
Cell lines | HepG2 cells |
Preparation Method | HepG2 cells were cultured in RPMi-1640 medium supplemented with 10% heat-inactivated calf serum, 100U/ml penicillin, and 100μg/ml streptomycin, and incubated at 37°C in a humidified environment with 5% CO2. HepG2 cells were seeded in 96-well plates, and 100μl of cells were added to each well (the cell density had been adjusted to 1×105/ml). Cells were allowed to adhere overnight and then exposed to medium and various concentrations of LYG-202 (0, 2, 5, and 8µM) for 24 hours. Subsequently, 20μl of MTT solution (5mg/ml) was transferred to each well to give a final assay volume of 220μl/well. The culture plates were incubated at 37°C and 5% CO2 for 4 hours. After incubation, the supernatant was removed, and 100μl DMSO was added to ensure complete dissolution of formazan crystals. The culture plate was placed on a fixed-rail oscillator for 2min, and absorbance was recorded at 562nm. |
Reaction Conditions | 0, 2, 5, and 8µM; 24h |
Applications | LYG-202 treatment significantly inhibited the viability of HepG2 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female BALB/c nude mice |
Preparation Method | Female BALB/c nude mice (35-40 days old, weighing 18-22g) were maintained in a pathogen-free environment (23±2°C, 55±5% humidity) on a 12h light-12h dark cycle, with food and water ad libitum throughout the experiment. Mice were subcutaneously inoculated with 5×106 MCF-7 cells per nude mouse. After 12-14 days, the tumor size was measured by micrometer, and then the nude mice with similar tumor volume were randomly divided into 3 groups (6 mice in each group): a saline tumor control group; (i.v.) wogonin 60mg/kg/2-day group; (i.v.) LYG-202 20mg/kg/2-day group. After 3 weeks, the nude mice were sacrificed, and the tumor xenografts were removed and measured. |
Dosage form | 20mg/kg/2-day for 3 weeks; i.v. |
Applications | LYG-202 treatment inhibited tumor growth in xenograft mice bearing MCF-7 tumors. |
References: | |
| Cas No. | 1175077-25-4 | SDF | |
| Canonical SMILES | CN1CCN(CCCCOC2=CC(O)=C(C(C=C(C3=CC=CC=C3)O4)=O)C4=C2OC)CC1 | ||
| 分子式 | C25H30N2O5 | 分子量 | 438.5 |
| 溶解度 | DMF: 14 mg/ml,DMF:PBS (pH7.2) (1:40): 0.12 mg/ml,Ethanol: 2.5 mg/ml | 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 | 2.2805 mL | 11.4025 mL | 22.805 mL |
| 5 mM | 456.1 μL | 2.2805 mL | 4.561 mL |
| 10 mM | 228.1 μL | 1.1403 mL | 2.2805 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。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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