GLPBio

LYG-202

Catalog No.: GC40865Purity:>98.00%
COASDSData Sheet
LYG-202 is a synthesized flavonoid with a piperazine substitution, exhibiting potent antitumor effects.

المنتجات مخصصة للاستخدام البحثي فقط، وليست للاستخدام البشري. نحن لا نبيع للمرضى.

LYG-202
Cas No.: 1175077-25-4
1mgIn Stock
$28.00
1
5mgIn Stock
$84.00
1
10mgIn Stock
$140.00
1
25mgIn Stock
$315.00
1
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المراجع (Citations)

لا تتوفر حاليًا مراجع لهذا المنتج. فيما يلي مجموعة مختارة من المنشورات التي تستشهد بمنتجات GlpBio.
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    187(9):2288-2304 (2024)
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الوصف (Description)

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.

البروتوكول (Protocol)

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:
[1] 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.
[2] 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.

وثائق المنتج (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

الخصائص الكيميائية (Chemical Properties)

رقم CAS
1175077-25-4
SMILES
CN1CCN(CCCCOC2=CC(O)=C(C(C=C(C3=CC=CC=C3)O4)=O)C4=C2OC)CC1
الصيغة الجزيئية
C25H30N2O5
الوزن الجزيئي
438.5
الذوبانية
DMF: 14 mg/ml,DMF:PBS (pH7.2) (1:40): 0.12 mg/ml,Ethanol: 2.5 mg/ml
التخزين
Store at -20°C
إرشادات عامة
اختر مذيبًا مناسبًا وفقًا لبيانات ذوبانية المنتج. بعد التحضير، قسّم المحلول المخزون إلى أجزاء لتجنب دورات التجميد والذوبان المتكررة.
استخدم المحاليل المخزونة خلال 6 أشهر عند حفظها في -80°C، أو خلال شهر واحد عند حفظها في -20°C.
لتحسين الذوبانية، سخّن الأنبوب إلى 37°C وعرّضه للموجات فوق الصوتية لمدة مناسبة.
شروط الشحن
تُشحن عينات التقييم مع عبوات تبريد. وتُشحن الأحجام الأخرى المتاحة في درجة حرارة الغرفة، أو مع عبوات تبريد عند الطلب.

الحاسبات (Calculators)المولارية / التخفيف / الوزن الجزيئي / تحويل الوحدات / تركيبة داخل الجسم الحي / الذوبانية

g/mol

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