| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
MG16 (48 hours) effectively inhibited the proliferation of LLC, A549 and H446 lung cancer cells in vitro, with IC50 values of 408.2 ± 32.4 nM, 613.1 ± 54.7 nM and 140.4 ± 10.4 nM, respectively [1]. Treatment with MG16 (0.1-100 nM; 48 hours) induced dose-dependent apoptosis in A549 and H446 lung cancer cells, and its pro-apoptotic activity in both cell lines was significantly stronger than that of SN-38 [1]. MG16 (concentration of 90.1-1 μM in A549 cells and 10-100 nM in H446 cells; treatment for 24 hours) regulated the expression of key apoptotic proteins and induced strong Caspase-3 activation in A549 and H446 lung cancer cells, with its Caspase-3 activation being more significant than that of SN-38 [1]. MG16 (613.1 nM; treatment for 48 hours) can induce cell cycle arrest in A549 lung cancer cells at its IC50 concentration in the G0/G1 phase [1].
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|---|---|
| ln Vivo |
MG16 (5 mg/kg; intravenous injection; every other day) achieved a tumor inhibition rate of 75.11% in a mouse LLC subcutaneous tumor model, demonstrating a potent inhibitory effect on lung cancer growth [1]. MG16 (5 mg/kg; intravenous injection; every other day) achieved a tumor inhibition rate of 80.5% in a mouse A549 subcutaneous tumor model, demonstrating a potent inhibitory effect on lung cancer growth [1].
|
| Cell Assay |
Western Blot Analysis [1]
Cell Types: A549 lung cancer cells, H446 lung cancer cells Tested Concentrations: 0.1-1 μM (A549 cells); 10-100 nM (H446 cells) Incubation Duration: 24 hours Experimental Results: In A549 cells, the pro-apoptotic protein Bax was upregulated, the anti-apoptotic protein Bcl-2 was downregulated, and caspase-3 was strongly activated. At both test concentrations, the level of cleaved caspase-3 was significantly higher than that in SN-38. In H446 cells, Bax was upregulated, Bcl-2 was downregulated, and caspase-3 was activated. At both test concentrations, the level of cleaved caspase-3 was significantly higher than that in SN-38, especially at the 100 nM concentration. |
| References |
| Molecular Formula |
C23H22CLN3O6
|
|---|---|
| Molecular Weight |
471.89
|
| CAS # |
2349329-01-5
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
CC[C@]1(C(OCC2=C1C=C3C4=NC5=CC=C(C=C5C=C4CN3C2=O)OC)=O)OC(CN)=O.Cl
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 2.1191 mL | 10.5957 mL | 21.1914 mL | |
| 5 mM | 0.4238 mL | 2.1191 mL | 4.2383 mL | |
| 10 mM | 0.2119 mL | 1.0596 mL | 2.1191 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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