| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
MRS8431 (0.1-25 μM; 20 min) effectively inhibited ABCG2-mediated ATPase activity in the cell membrane of High-Five insects, with an IC50 value of 0.16 μM, showing significant inhibitory effects at concentrations of 1 μM and above [1]. MRS8431 (0.1-25 μM; 20 min) had no significant effect on P-gp-mediated ATPase activity at concentrations up to 1 μM, and only showed partial inhibitory effects at high concentrations (10 and 25 μM) [1]. MRS8431 (0-2.5 μM) effectively inhibited the transport of ABCG2-mediated mitoxantrone (IC50 of 0.50 μM) and pheophytic acid A (IC50 of 0.88 μM) in HEK293 R-5 cells expressing ABCG2 [1]. MRS8431 (10 μM) showed only a slight partial inhibitory effect on P-gp-mediated BD-verapamil transport in P-gp-expressing HeLa-S3 cells (inhibition rate of 35.4% at 10 μM) [1]. MRS8431 (concentration up to >25 μM; treatment for 72 hours) was cytotoxic to both HEK293-pcDNA control cells (IC50 of 2.20 μM) and HEK293 R-5 cells expressing ABCG2 (IC50 of 1.98 μM) and was not transported by ABCG2 [1]. MRS8431 (0.6 μM; treatment for 72 hours) significantly enhanced the sensitivity of HEK293 R-5 cells expressing ABCG2 to mitoxantrone, reduced the IC50 value of mitoxantrone, and eliminated ABCG2-mediated chemotherapy resistance [1].
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|---|---|
| Cell Assay |
Cytotoxicity assay [1]
Cell Types: HEK293-pcDNA control cells; HEK293 R-5 cells expressing ABCG2 Tested Concentrations: >25 μM Incubation Duration: 72 hours Experimental Results: The IC50 in HEK293-pcDNA control cells was 2.20 μM. The IC50 in HEK293 R-5 cells expressing ABCG2 was 1.98 μM. The survival curves of the control cells and the cells expressing ABCG2 overlapped, indicating that the compound is not a substrate of ABCG2. |
| References |
| Molecular Formula |
C36H28CLF2N9O3
|
|---|---|
| Molecular Weight |
708.12
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O[C@@H]1[C@H](O)[C@](C(NC)=O)(C2)[C@H]2[C@H]1N(C=N3)C4=C3C(NCC5=CC=C(C=C5)N6N=NC(C7=CC=C(C=C7)Cl)=C6)=NC(C#CC8=CC=C(C(F)=C8)F)=N4
|
| 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)
|
| 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 | 1.4122 mL | 7.0610 mL | 14.1219 mL | |
| 5 mM | 0.2824 mL | 1.4122 mL | 2.8244 mL | |
| 10 mM | 0.1412 mL | 0.7061 mL | 1.4122 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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