| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
MST3-IN-1 (compound LD-1) showed anti-proliferative activity against various cancer cell lines, with GI50 values of 0.68 μM (HepG2 cells), 0.77 μM (HCT116 cells), and 0.83 μM (H226 cells), respectively. The inhibitory concentrations against HK2 cells were all greater than 30 μM, showing good selectivity [1]. MST3-IN-1 (1 μM) inhibited MST3 by 95.49%, while the inhibition rate against the second-ranked kinase AKT2 was only 66.51% [1]. MST3-IN-1 (0.25-2 μM, 24 h) could induce apoptosis in HepG2 cells and may inhibit HepG2 cell proliferation by prolonging the G2/M phase [1]. MST3-IN-1 (0.25-2 μM, 24 h) reduced the expression level of p-MST3 in a concentration-dependent manner, but did not affect the expression level of MST3 [1].
|
|---|---|
| ln Vivo |
MST3-IN-1 (compound LD-1) (40 mg/kg, once daily for 15 days) showed good efficacy in inhibiting the growth of hepatocellular carcinoma tumors in HepG2 xenograft mice [1].
|
| Cell Assay |
Apoptosis analysis [1]
Cell Types: HepG2 cells Tested Concentrations: 0.5, 1, 2 μM Incubation Duration: 24 hours Experimental Experimental Results: Induced apoptosis in HepG2 cells. Immunofluorescence [1] Cell Types: HepG2 cells Tested Concentrations: 0.5, 1, 2 μM Incubation Duration: 48 hours Results revealed unique morphological features of apoptosis, including chromatin condensation and nuclear fragmentation. Cell cycle analysis [1] Cell Types: HepG2 cells Tested Concentrations: 0.25, 0.5, 1 μM Incubation Duration: 24 hours Experimental Results: Increased the proportion of G2/M phase cells.
|
| Animal Protocol |
Animal/Disease Models:HepG2 cells (5 × 10⁶) were subcutaneously injected into the right axilla of mice [1].
Doses: 40 mg/kg. Route of Administration: Daily gavage for 15 consecutive days. Experimental Results: The tumor growth inhibition rate (TGI) significantly reached 47.64%, which was superior to the current first-line treatment drug sorafenib (TGI = 32.52%). No deaths or significant weight loss were observed in mice in any of the dosage groups. |
| References |
| Molecular Formula |
C25H21F4N5O3S
|
|---|---|
| Molecular Weight |
547.52
|
| CAS # |
3095435-97-2
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(C1=CN(C2CC2)C3=CC(N4CCNCC4)=C(C=C3C1=O)F)NC5=NC6=C(S5)C=C(OC(F)(F)F)C=C6
|
| 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 | 1.8264 mL | 9.1321 mL | 18.2642 mL | |
| 5 mM | 0.3653 mL | 1.8264 mL | 3.6528 mL | |
| 10 mM | 0.1826 mL | 0.9132 mL | 1.8264 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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