| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
MEDS700 (0.001-10 μM; 3 days) can induce differentiation and apoptosis in THP1 and U937 acute myeloid leukemia (AML) cell lines, with EC50 values ranging from 19 nM to 64 nM [1]. MEDS700 (0.1-1 μM; 3 days) can induce apoptosis in MV4-11 acute myeloid leukemia (AML) cells at concentrations of 0.1 μM and 1 μM [1]. MEDS700 has shown potent antiproliferative activity against a variety of solid tumor cell lines at nanomolar concentrations, with the strongest activity against neuroblastoma, Ewing's sarcoma, bladder cancer and fibrosarcoma cells [1]. MEDS700 can effectively inhibit the proliferation of SF7761 and SU-DIPG-XIII DMG cell lines, with EC50 values of 9.3 nM and 32.9 nM, respectively, and also showed activity against SF8628 cells after prolonged exposure time [1]. MEDS700 (72 h) exerted antiproliferative and cytotoxic effects on SH-SY5Y neuroblastoma cells through pyrimidine depletion, inducing S-phase cell cycle arrest, caspase-dependent apoptosis, and irreversible loss of colony-forming ability, with an EC50 value of 13 nM [1]. MEDS700 (1-100 μM; 72 h) showed only very low toxicity in a mixed neural cell culture derived from human induced pluripotent stem cells (hiPSCs), with an EC30 of 199 μM, indicating that the compound has a good safety window relative to its antitumor activity [1].
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|---|---|
| ln Vivo |
MEDS700 (5-20 mg/kg; intravenous injection, oral administration; single dose) exhibits good oral bioavailability, sustained systemic exposure and effective blood-brain barrier penetration, with brain concentrations remaining above the in vitro anticancer EC50 range for 24 hours after oral administration [1].
|
| Cell Assay |
Apoptosis Analysis [1]
Cell Types: MV4-11 AML Cells Tested Concentrations: 0.1 μM, 1 μM Incubation Duration: 3 days Experimental Results: Approximately 40% apoptosis was induced at both 0.1 μM and 1 μM concentrations. Co-treatment with 5 μM uridine reduced apoptosis. Co-treatment with dipyridamole (1.0 μM) increased apoptosis to approximately 100% at both concentrations, even in the presence of 5 μM or 100 μM uridine. |
| Animal Protocol |
Animal/Disease Models:Balb/c (male, 8 weeks old) [1]
Doses: 5 mg/kg (intravenous); 20 mg/kg (oral) Route of Administration: Intravenous; single dose; oral; single dose Experimental Results: Oral bioavailability was 37.8%. The half-life after oral administration was more than 12 hours, and the half-life after intravenous administration was 8.1 hours. The brain Cmax was 0.67 μg/mL. After oral administration, the brain drug concentration was maintained at about 160 nM for up to 24 hours, which is therapeutic. |
| References |
| Molecular Formula |
C23H15F6N3O3
|
|---|---|
| Molecular Weight |
495.37
|
| CAS # |
2770979-81-0
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
FC1=C(F)C(NC(C2=C3C=CC=CN3N=C2O)=O)=C(F)C(F)=C1C4=CC(OCC(F)(F)C)=CC=C4
|
| 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
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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 | 2.0187 mL | 10.0935 mL | 20.1869 mL | |
| 5 mM | 0.4037 mL | 2.0187 mL | 4.0374 mL | |
| 10 mM | 0.2019 mL | 1.0093 mL | 2.0187 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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