Size | Price | |
---|---|---|
100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
EZH2 EZH2 490 nM (IC50) BRD4 34 nM (IC50)
|
---|---|
ln Vitro |
Compound D7, YM458 (0-30 μM; 6 days) exhibits antiproliferative properties against AsPC-1 cells, with an IC50 of 0.69 ± 0.16 μM. Additionally, exposure to 1 μM for 72 hours dramatically reduces the levels of c-Myc and H3K27me3 in AsPC-1[1]. YM458 (0-30 μM; 4 or 6 days) strongly decreases the growth of A549 lung cancer cells and HCT116 colorectal cancer cells at 1 μM, as well as a variety of other solid cancer cell types[1]. AsPC-1, HCT116, and A549 cancer cell colony formation is inhibited in a dose-dependent manner by YM458 (0.05-0.4 μM; 12-20 days)[1].
|
ln Vivo |
YM458 (60 mg/kg; IP; every other day, for 38 days) inhibits the formation of tumors in AsPC-1 cells by 38.6% and in A549 cells by 62.3%[1]. Female BALB/c mice's pharmacokinetic parameters for YM458[1]. AUC0-24 (ng/mL·h) 27126.3 4383.6 IP (80 mg/kg) PO (80 mg/kg) t1/2 (h) 3.81 4.16 Tmax (h) 1 1 Cmax (ng/mL) 273220.1 13509.1 CL (mL/min/kg) 4.88 F (%) 4.94
|
Cell Assay |
Western Blot Analysis
Cell Types: AsPC-1[1] Tested Concentrations: 1 μM Incubation Duration: 72 hrs (hours) Experimental Results: diminished the degree of H3K27me3 and c-Myc Dramatically. Cell Proliferation Assay Cell Types: AsPC -1, SW1990, CFPAC-1, A549, HCC827, H1650, H292, H460, DLD1, HCT116, and RKO[1] Tested Concentrations: 0-30 μM Incubation Duration: 4 or 6 days Experimental Results: Inhibited cell proliferation on a broad range of solid cancer cells, and Dramatically suppressed proliferation of A549 lung cancer cells and HCT116 colorectal cancer cells at 1 μM. |
Animal Protocol |
Animal/Disease Models: BALB/c nude mice (injected with A549 or AsPC-1 )[1]
Doses: 60 mg/kg Route of Administration: IP; every other day, for 38 days Experimental Results: Prevented tumor growth with inhibitory rates of 38.6% in AsPC-1 cells and 62.3% in A549 cells. |
References |
[1]. Guo Z, et al. Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors. J Med Chem. 2022;65(9):6573-6592.
|
Molecular Formula |
C53H61CLN8O5S
|
---|---|
Molecular Weight |
957.62
|
CAS # |
2770108-93-3
|
Appearance |
Typically exists as solids (or liquids in special cases) 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 | 1.0443 mL | 5.2213 mL | 10.4426 mL | |
5 mM | 0.2089 mL | 1.0443 mL | 2.0885 mL | |
10 mM | 0.1044 mL | 0.5221 mL | 1.0443 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.