| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
P-gp inhibitor 30 (compound A38) (0.1 μM) reversed ADM resistance in MDA-MB-231/ADM cells and significantly reduced the IC50 value of ADM from 785.46 μM to 2.05 μM [1]. P-gp inhibitor 30 (0.125-4 μM) significantly inhibited the activity of P-gp ATPase at different concentrations in a concentration-dependent manner [1]. P-gp inhibitor 30 interacts with P-gp, inhibiting its function without downregulating its expression and stabilizing the protein, thereby reducing its degradation in MCF7/ADM cells under elevated temperature conditions [1]. P-gp inhibitor 30 (6 h) significantly increased the expression intensity of Rh123 in MCF7/ADM cells and increased the accumulation of ADM in MDA-MB-231/ADM cells, while inhibiting the efflux of Rh123 [1]. When P-gp inhibitor 30 (0.1-1 μM, 24 hours-15 days) was used in combination with ADM, it promoted apoptosis of drug-resistant breast cancer cells (MCF7/ADM and MDA-MB-231/ADM cells), inhibited cell proliferation, migration and invasion, indicating that it could enhance the sensitivity of these cells to ADM[1]. When P-gp inhibitor 30 (0.1 μM) was used in combination with ADM, it led to the accumulation of autophagosomes in MCF7/ADM and MDA-MB-231/ADM cells and significantly increased the expression of autophagy-related proteins, thereby inducing cell death[1]. When P-gp inhibitor 30 (1-10 days) was used in combination with ADM, it significantly reduced the tumor volume of MCF7/ADM and MDA-MB-231/ADM cells in a 3D tumor spheroid model[1].
|
|---|---|
| ln Vivo |
When P-gp inhibitor 30 (2 mg/kg, intraperitoneal injection, once every 2 days for 14 days) was used in combination with ADM, it showed antitumor effects in the MCF-7/ADM model [1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: MCF7/ADM and MDA-MB-231/ADM cells Tested Concentrations: 0.1 μM Incubation Duration: 24 h Experimental Results: Significantly increases the expression level of LC3 when combined with ADM. Apoptosis Analysis[1] Cell Types: MCF7/ADM and MDA-MB-231/ADM cells Tested Concentrations: 0.1, 0.5 and 1 μM Incubation Duration: 48 h Experimental Results: Significantly increased ADM-induced apoptosis in a dose-dependent manner compared to the MCF7/ADM control group. Significantly increased ADM-induced apoptosis on MDA-MB-231/ADM cells. Cell Proliferation Assay[1] Cell Types: MCF7/ADM and MDA-MB-231/ADM cells Tested Concentrations: 0.1, 0.5 and 1 μM Incubation Duration: 15 days Experimental Results: Significantly inhibited the proliferation of MCF7/ADM cells in a dose-dependent manner compared to the MCF7/ ADM control group when combined with ADM. Resulted in only a few cells survived at a concentration of 1 μM. Markedly inhibited the proliferation of drug-resistant breast cancer cells when combined with ADM. Cell Migration Assay [1] Cell Types: MCF7/ADM and MDA-MB-231/ADM cells Tested Concentrations: 0.1 μM Incubation Duration: 36 h Experimental Results: Suppressed the migration ability of breast cancer drug- resistant cells when combined with ADM. Cell Invasion Assay[1] Cell Types: MCF7/ADM and MDA-MB-231/ADM cells Tested Concentrations: 0.1 μM Incubation Duration: 24 h Experimental Results: Suppressed the invasion ability of breast cancer drug- resistant cells when combined with ADM. |
| Animal Protocol |
Animal/Disease Models: Female BALB/c nude mice (4-5 weeks old) subcutaneously injected with MCF-7/ADM cells[1]
Doses: 2 mg/kg Route of Administration: i.p., every 2 days for 14 days Experimental Results: Significantly reduced tumor size when combined with ADM (10 mg/kg), with efficacy comparable to Tariquidar. Showed significantly lower tumor weight than that of other groups. Showed no significant loss compared to control. Caused no significant tissue cell necrosis. |
| References |
| Molecular Formula |
C22H15FN4O2
|
|---|---|
| Molecular Weight |
386.38
|
| Appearance |
Typically exists as solids at room temperature
|
| 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 | 2.5881 mL | 12.9406 mL | 25.8813 mL | |
| 5 mM | 0.5176 mL | 2.5881 mL | 5.1763 mL | |
| 10 mM | 0.2588 mL | 1.2941 mL | 2.5881 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
