| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PRMT1-IN-3 (Compound YH-4) (10 μM, 37-65°C) significantly enhanced the thermal stability of PRMT1 (ΔTm = +5.2°C) but had no significant effect on other PRMT subtypes [1]. PRMT1-IN-3 (0.01-100 μM, 48 h) inhibited the growth of MDA-MB-231, HCT116, HeLa and A549 cells, with IC50 values of 6.38 μM, 15.29 μM, 12.97 μM and 9.187 μM, respectively [1]. PRMT1-IN-3 (1.25-10 μM, 48 h) inhibited ADMA levels and H4R3me2a modification in MDA-MB-231 cells in a dose-dependent manner [1]. PRMT1-IN-3 (0-20 μM, 72 h) (resistance index: 9.0) showed synergistic effects with Paclitaxel (PTX) (resistance index: 92.7) in MDA-MB-231 cells and MDA-MB-231/Taxol cells [1]. PRMT1-IN-3 (0-40 μM, 0-48 h) induced G0/G1 phase arrest and apoptosis, and inhibited cell migration of MDA-MB-231 cells [1]. PRMT1-IN-3 (0-20 μM, 10 d) almost completely inhibited colony formation of MDA-MB-231 cells at a concentration of 20 μM [1].
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| ln Vivo |
PRMT1-IN-3 (compound YH-4) (30 mg/kg, intraperitoneal injection, for one week followed by a three-day break, for a total of 21 days) is a chemosensitizer of PTX that enhances its therapeutic effect while significantly reducing the required dose and alleviating its toxic side effects in the TNBC model [1].
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| Cell Assay |
Apoptosis Analysis[1]
Cell Types: MDA-MB-231 cells Tested Concentrations: 0, 5, 20 and 40 μM Incubation Duration: 48 h Experimental Results: Resulted in an increase in early apoptosis from 2.34 % to 34.3 % from 2.5 μM to 40 μM. Cell Cycle Analysis[1] Cell Types: MDA-MB-231 cells Tested Concentrations: 0, 2.5, 5, 10, 20 μM Incubation Duration: 48 h Experimental Results: Observed that the proportion of cells in the G0/G1 phase increased in a dose-dependent manner from 41.8 % to 60.9 %, while the proportions of cells in the S phase and G2/M phase decreased in a dose-dependent manner from 33.2 % to 23.6 % and from 24.9 % to 15.2 %, respectively. Cell Migration Assay [1] Cell Types: MDA-MB-231 cells Tested Concentrations: 1.25, 2.5, 5, 10 and 20 μM Incubation Duration: 0, 12, 36, and 48 h Experimental Results: Decreased the healing rate to 18.52% after 48 h at 20 μM. |
| Animal Protocol |
Animal/Disease Models: MDA-MB-23-YFP-Luc cells induced xenograft model established in female nude mice 4-5 weeks old weighing 16-18 g[1]
Doses: 30 mg/kg with or without PTX Route of Administration: Intraperitoneal injection (i.p.), for one week, then discontinue for three days, for a total of 21 days Experimental Results: Demonstrated significant inhibitory effects on tumor volume, with the combination of PTX showing a markedly superior antitumor efficacy compared to the monotherapies. |
| References |
| Molecular Formula |
C18H23FN2O
|
|---|---|
| Molecular Weight |
302.39
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| CAS # |
892570-48-8
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| Appearance |
Typically exists as solids at room temperature
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| 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)
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| 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 | 3.3070 mL | 16.5349 mL | 33.0699 mL | |
| 5 mM | 0.6614 mL | 3.3070 mL | 6.6140 mL | |
| 10 mM | 0.3307 mL | 1.6535 mL | 3.3070 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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