| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
NSD2/H3K36me2 modulator-1 (Compound 5b) (24 hours) showed inhibitory activity of IC50 < 5 μM against all five cancer cell lines (IC50 values of 4.67, 2.12, 2.64, 4.56 and 4.99 μM in A549, HepG-2, PC-3, HCT-116 and MCF-7 cells, respectively), confirming its excellent broad-spectrum antitumor activity [1]. NSD2/H3K36me2 modulator-1 showed higher tumor selectivity for HepG-2 cells than for HaCaT cells (IC50 = 19.2 μM) (selectivity index (SI) = 9.06) [1]. NSD2/H3K36me2 modulator-1 (2 μM, 24 hours, 37-62℃) effectively bound to NSD2 in HepG-2 cells [1]. NSD2/H3K36me2 modulator-1 (2, 4 μM, 24 h) inhibits NSD2 and selectively downregulates NSD2-mediated H3K36me2 in HepG-2 cells[1]. NSD2/H3K36me2 modulator-1 (2, 4 μM, 24 h) reverses EMT at the molecular level, which may be achieved by inhibiting NSD2 and subsequently downregulating TWIST1, resulting in altered expression of key regulators of epithelial-mesenchymal transition (EMT)[1]. NSD2/H3K36me2 modulator-1 (2, 4 μM, 18, 36 h) significantly inhibits the migration and proliferation of HepG-2 cells[1]. NSD2/H3K36me2 modulator-1 (2, 4 μM, 24 h) has multiple regulatory effects on HepG-2 cells, including effectively inducing apoptosis, triggering concentration-dependent G0/G1 phase arrest, dose-dependent reduction of mitochondrial membrane potential (MMP), and effectively promoting ROS production [1].
|
|---|---|
| ln Vivo |
NSD2/H3K36me2 modulator-1 (Compound 5b) (20, 40 mg/kg, daily vascular wall, for 18 consecutive days) showed strong anti-tumor effects in the HepG-2 cell xenograft model, effectively inhibiting tumor growth and with good safety, indicating that there were no significant differences in body weight, organ index and morphological characteristics [1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: HepG-2 cells Tested Concentrations: 2, 4 μM Incubation Duration: 24 h Experimental Results: Suppressed NSD2 expression in a dose-dependent manner, with notably strong inhibition at 4 μM. Exhibited high selective inhibition of H3K36me2. Bound effectively to NSD2 within cells. Apoptosis Analysis[1] Cell Types: HepG-2 cells Tested Concentrations: 2, 4 μM Incubation Duration: 24 h Experimental Results: Significantly increased the total apoptosis rate in HepG-2 cells with the elevation of the concentration. Exhibited slightly superior apoptosis-inducing capacity at the concentration of 4 μM. Western Blot Analysis[1] Cell Types: HepG-2 cells Tested Concentrations: 2, 4 μM Incubation Duration: 24 h Experimental Results: Significantly suppressed TWIST1 expression. Dose-dependently downregulated N-Cadherin and Vimentin. Upregulated E-Cadherin and Occludin in a dose-dependent manner. Cell Cycle Analysis[1] Cell Types: HepG-2 cells Tested Concentrations: 0, 2, 4 μM Incubation Duration: 24 h Experimental Results: Elevated the proportion of HepG-2 cells in G0/G1 phase from 53.8 % to 65.7 %, with the concentration increasing from 0 to 2 μM. Increased the G0/G1 subpopulation to 79.6 %, with the concentration reaching 4 μM, and exceeded that of 5-Fluorouracil (73.5 %). Induced a marked decrease in the levels of cell cycle regulators CDK2, CDK4, and CDK6, effectively blocking cell cycle progression in a concentration-dependent manner. |
| Animal Protocol |
Animal/Disease Models: An HepG-2 xenograft model established in female BALB/c nude mice (6-8 weeks old)[1]
Doses: 20, 40 mg/kg Route of Administration: daily oral gavage (p.o.) for 18 consecutive days Experimental Results: Significantly suppressed tumor growth in a dose-dependent manner. Exhibited the strongest antitumor effect at 40 mg/kg. |
| References |
| Molecular Formula |
C41H59CLN2O5
|
|---|---|
| Molecular Weight |
695.37
|
| 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 | 1.4381 mL | 7.1904 mL | 14.3808 mL | |
| 5 mM | 0.2876 mL | 1.4381 mL | 2.8762 mL | |
| 10 mM | 0.1438 mL | 0.7190 mL | 1.4381 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
