| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
LYG-202 targets multiple pathways involved in cancer progression. It inhibits VEGF-induced angiogenesis by suppressing endothelial cell migration and tube formation. Additionally, LYG-202 inhibits BRD4, a bromodomain-containing protein that regulates gene expression by binding to acetylated histones and altering chromatin structure. By inhibiting BRD4, LYG-202 modulates the expression of genes involved in cell proliferation and survival. The compound's dual mechanism of action—targeting both angiogenesis and epigenetic regulation—makes it a promising anticancer agent.
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| ln Vitro |
In vitro, LYG-202 effectively inhibits VEGF-induced endothelial cell migration and tube formation in HUVEC (human umbilical vein endothelial cell) models. The compound also inhibits BRD4 function, a BET protein that regulates gene expression by altering chromatin structure. By targeting both angiogenesis and epigenetic regulation, LYG-202 modulates the expression of genes involved in cell proliferation and survival. The compound's anti-angiogenic and antitumor activities make it a valuable tool for cancer research.
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| ln Vivo |
In vivo activity data for LYG-202 are limited. Based on its potent in vitro anti-angiogenic and antitumor activities, the compound is expected to demonstrate antitumor efficacy in animal models of cancer by suppressing tumor-associated angiogenesis and modulating gene expression. Typical in vivo studies for this class of compounds involve administration to tumor-bearing mouse models, with assessment of tumor growth inhibition and angiogenesis markers.
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| Enzyme Assay |
For non-cellular in vitro assays, LYG-202 is evaluated for its binding affinity to BRD4 and other BET proteins. The compound is incubated with purified BRD4 bromodomain, and binding is measured using surface plasmon resonance, isothermal titration calorimetry, or fluorescence polarization assays. The compound's ability to inhibit VEGF signaling may be assessed in cell-free angiogenesis assays.
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| Cell Assay |
For in vitro cellular assays, LYG-202 is tested in HUVEC models to assess its anti-angiogenic activity. HUVEC cells are treated with the compound in the presence of VEGF, and endothelial cell migration is assessed using transwell or scratch wound healing assays. Tube formation is assessed by plating HUVEC cells on Matrigel and measuring tube-like structure formation. The compound's effects on BRD4 function are assessed in cancer cell lines by measuring gene expression changes and cell proliferation.
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| Animal Protocol |
For in vivo animal studies, LYG-202 would typically be evaluated in xenograft mouse models of cancer. Mice bearing established tumors are treated with the compound at various doses via oral or intraperitoneal administration. Tumor volumes are measured regularly, and tumor growth inhibition is calculated. Angiogenesis markers (such as CD31 staining) and BRD4 target gene expression are assessed in tumor tissues at study endpoint. Body weight and general health are monitored to evaluate tolerability.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for LYG-202 are limited. As a small-molecule flavonoid with a molecular weight of 438.52, it is expected to have moderate oral bioavailability and tissue distribution. The compound is soluble in DMSO and can be formulated for in vivo administration. Further pharmacokinetic studies would be needed to determine its absorption, distribution, metabolism, and excretion profile. The compound is for research use only and not for human use.
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| Toxicity/Toxicokinetics |
Toxicological data for LYG-202 are limited. As a compound that inhibits both angiogenesis and BRD4 function, it may have on-target effects on normal angiogenesis and gene regulation. Comprehensive toxicology studies including acute and repeat-dose toxicity, genotoxicity, and organ-specific toxicity assessments would be required for therapeutic development. The compound is for research use only and not for human use.
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| References |
[1]. Chen Y, et al. LYG-202, a newly synthesized flavonoid, exhibits potent anti-angiogenic activity in vitro and in vivo. J Pharmacol Sci. 2010;112(1):37-45.
[2]. Zhao Y, et al. LYG-202 exerts antitumor effect on PI3K/Akt signaling pathway in human breast cancer cells. Apoptosis. 2015 Sep;20(9):1253-69. |
| Additional Infomation |
LYG-202 is a synthetic flavonoid compound exhibiting potent anti-angiogenic and antitumor activity. It effectively inhibits VEGF-induced endothelial cell migration and tube formation in HUVEC models and inhibits BRD4 function, a BET protein that regulates gene expression by altering chromatin structure. LYG-202 modulates the expression of genes involved in cell proliferation and survival and has a molecular weight of 438.52 with molecular formula C₂₅H₃₀N₂O₅.
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| Molecular Formula |
C25H30N2O5
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|---|---|
| Molecular Weight |
438.52
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| Exact Mass |
438.215
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| CAS # |
1175077-25-4
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| PubChem CID |
44156930
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.456
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
32
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| Complexity |
642
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(C2=CC=CC=C2)OC2=C(OC)C(OCCCCN3CCN(C)CC3)=CC(O)=C2C(=O)C=1
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| InChi Key |
ICGYSEWPMDWBIL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H30N2O5/c1-26-11-13-27(14-12-26)10-6-7-15-31-22-17-20(29)23-19(28)16-21(18-8-4-3-5-9-18)32-25(23)24(22)30-2/h3-5,8-9,16-17,29H,6-7,10-15H2,1-2H3
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| Chemical Name |
5-hydroxy-8-methoxy-7-[4-(4-methylpiperazin-1-yl)butoxy]-2-phenylchromen-4-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 5 mg/mL (11.40 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2804 mL | 11.4020 mL | 22.8040 mL | |
| 5 mM | 0.4561 mL | 2.2804 mL | 4.5608 mL | |
| 10 mM | 0.2280 mL | 1.1402 mL | 2.2804 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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