| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
OXPHOS-IN-2 (compound 28c) (0-1000 μM, 12 h) reduced the ATP to NAD+/NADH ratio in PC9 cells and inhibited AMPK phosphorylation [1]. OXPHOS-IN-2 (0-20 nM, 14 days) significantly inhibited the colony-forming ability of PC9 cells [1]. OXPHOS-IN-2 (0-1 μM) induced apoptosis in PC9 and Bxpc-3 cells by dose-dependently increasing reactive oxygen species (ROS) levels and decreasing mitochondrial membrane potential [1]. OXPHOS-IN-2 (0-50 nM) induced DNA damage in PC9 cells and increased γ-H2AX expression [1]. OXPHOS-IN-2 inhibited the proliferation of various tumor cell lines in glucose and galactose media, including H1975 (IC50 = 6.43 nM and 29.5 nM), H2228 (IC50 = 4.54 nM and 21.5 nM), KP-4 (IC50 = 3.61 nM and 48.7 nM), MKN45 (IC50 = 5.78 nM and 29.8 nM), HCT116 (IC50 = 5.19 nM and 31.2 nM), MDA-MB-231 (IC50 = 1.31 nM and 7.5 nM), MHCC-97H (IC50 = 1.76 nM and 12.4 nM), and SiHA (IC50 = 5.10 nM and 12.4 nM). 35.1 nM) cells[1].
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|---|---|
| ln Vivo |
OXPHOS-IN-2 (compound 28c) (7.5 mg/kg; orally; once daily for 14 days) significantly inhibited tumor growth in male BALB/c-nu mice with PC9 model and had good safety [1].
|
| Cell Assay |
Apoptosis analysis [1]
Cell Types: PC9 spheroids Tested Concentrations: 1, 10, 20 nM Incubation Duration: 72 hours Experimental Experimental Results: Significantly increased the apoptosis rate of cells. Western Blot analysis [1] Cell Types: PC9 cells Tested Concentrations: 1, 10, 50 nM Incubation Duration: 12 hours Experimental Results: Significantly reduced pAMPK levels. |
| Animal Protocol |
Animal/Disease Models:5 × 10⁷ PC9 cells were injected into male BALB/c-nu mice (3-4 weeks) [1]
Doses: 7.5 mg/kg Route of Administration: Oral (po); once daily for 14 days Experimental Results: Significantly inhibited tumor volume and tumor weight, superior to IACS-010759. No significant changes in body weight were observed. Significantly reduced the NAD⁺/NADH ratio and ATP content. |
| References |
| Molecular Formula |
C27H27F3N6O4S
|
|---|---|
| Molecular Weight |
588.60
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
FC(F)(F)OC1=CC=C(C2=NOC(C3=NN(CC4=CC=CC(N5CCC(S(=O)(C)=O)CC5)=C4)C(C6CC6)=N3)=N2)C=C1
|
| 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 | 1.6989 mL | 8.4947 mL | 16.9895 mL | |
| 5 mM | 0.3398 mL | 1.6989 mL | 3.3979 mL | |
| 10 mM | 0.1699 mL | 0.8495 mL | 1.6989 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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