| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Gipavalin (compound 8) (72 hours) inhibited the proliferation of human tumor cell lines (IC50: 5.7 μM for SHSY5Y, 6.3 μM for HL-60, 9.2 μM for K562, 9.8 μM for HT-1080, and 11.5 μM for A-549) [1]. Gipavalin (8 μM, 24-72 hours) arrested the cell cycle of HL-60 cells at the G1 phase and induced caspase-independent apoptosis [1]. Gipavalin (72 hours) completely inhibited drug-resistant cell lines and was not affected by transport proteins that mediate the efflux of antitumor drugs [1]. Gipavalin (1 μM, 24 hours) inhibited the invasive ability of HOS and 143B cells [2]. Gepavalin (0.5-2 μM, 24-48 hours) can activate the apoptosis pathway in HOS and 143B cells, inhibit COX2 and its downstream angiogenesis pathway, and induce caspase-dependent apoptosis [2]. Gepavalin exerts an antitumor effect in osteosarcoma cells by downregulating COX2, while COX2 overexpression reverses its inhibitory effect on cell proliferation and invasion [2]. Gepavalin (10 μM, 24 hours) can disrupt the cytoskeleton of Balb/c 3T3 fibroblasts, especially intermediate filaments [3]. The inhibition rate of MAO-B extracted from rat liver mitochondria by gepavalin (0.01-10 μM) increased significantly with increasing concentration, pIC50 = 6.84 (IC50 = 1.45 μM) [4].
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| ln Vivo |
Geiparvarin (compound 8) (0.5 mg/kg, intraperitoneal injection, every three days for several weeks/once daily) inhibited tumor growth and lung metastasis in a nude mouse 143B/9901 cell xenograft tumor model without significant toxicity [2].
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| Cell Assay |
Cell viability assay [1]
Cell Types: K562 cells, HL-60 cells, HT-1080 cells, A-549 cells, SHSY5Y cells, CEM cells, CEM/Vbl100 cells, LoVo cells, LoVo/Doxo cells; Tested Concentrations: Incubation Duration: 72 hours Experimental Results: The IC50 range in human tumor cell lines was 5.7 μM-11.5 μM. Cytotoxicity assay [5] Cell Types: L02 cells, A-549 cells, HeLa cells, QGY-7701 cells, SW480 cells, SGC7901 cells, MDA-MB-231 cells Tested Concentrations:Incubation Duration: 48 hours Experimental Results: It has significant inhibitory activity against a variety of cancer cells (e.g., SGC7901: IC₅₀=7.59 μM; HeLa: IC₅₀=9.09 μM), and low toxicity to normal hepatocytes L02 (IC₅₀>300 μM). The IC₅₀ values of the treated cells ranged from 7.59 to 20.34 μM. Apoptosis Analysis [1][2] Cell Types: HOS cells, 143B cells, HL-60 cells Tested Concentrations: HOS cells and 143B cells: 0.5 μM, 1 μM, 2 μM; HL-60 cells: 8 μM Incubation Duration: HOS cells and 143B cells: 24 hours, 48 hours; HL-60 cells: 72 hours Experimental Results: Significantly increased Caspase-3 enzyme activity. After 72 hours, the proportion of G1 phase cells decreased from 43.7% to 34.8%. Induced DNA fragmentation in HL-60 cells. Electron microscopy revealed that this method led to chromatin condensation and apoptotic body formation in HL-60 cells.
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| Animal Protocol |
Animal/Disease Models:Female nude mouse 143B/9901 cell xenograft tumor model (6 weeks) [2]
Doses: 0.5 mg/kg Route of Administration: Intraperitoneal injection (ip), once every 3 days for several weeks; Intraperitoneal injection (ip), once daily (for safety assessment) Experimental Results: Significantly reduced tumor volume and weight in the subcutaneous xenograft model and increased apoptotic cells in tumor tissue. Inhibited the growth of primary tumors and lung metastases and reduced the number and size of lung metastatic nodules. Increased mouse body weight without pathological damage to major organs. |
| References |
|
| Molecular Formula |
C19H18O5
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|---|---|
| Molecular Weight |
326.34
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| CAS # |
36413-91-9
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
C/C(C(OC(C)1C)=CC1=O)=C\COC2=CC=C(C=CC(O3)=O)C3=C2
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.0643 mL | 15.3214 mL | 30.6429 mL | |
| 5 mM | 0.6129 mL | 3.0643 mL | 6.1286 mL | |
| 10 mM | 0.3064 mL | 1.5321 mL | 3.0643 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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