| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| Targets |
IC50: 8.6 nM (EZH2); 62 nM (EZH1)[1]. DC50: 140 nM (EZH2 in MDA-MB-453 cells)[1]
|
|---|---|
| ln Vitro |
MS8815 demonstrates effectiveness in blocking the methyltransferase activity of EZH2 and EZH1 with IC50 values of 8.6 nM and 62 nM, respectively[1]. In MDA-MB-453 cells, MS8815 (0.1–1 μM) destroys EZH2 with a DC50 value of 140 nM[1]. In TNBC cells, MS8815 (1 μM; 48 h) causes substantial EZH2 degradation in a manner that is dependent on concentration, time, and proteasome activity[1]. Multiple TNBC cell lines and primary patient TNBC cells exhibit efficient growth suppression when treated with MS8815 (0.1-10 μM; 5 days)[1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: MDA-MB-453 cells and BT549 cells Tested Concentrations: 0.3, 3 μM; 1μM Incubation Duration: 48 h; 24 h Experimental Results: Induced nearly complete degradation of EZH2 and demonstrated the most robust degradation at 0.3 μM. Induced EZH2 degradation in a time-and concentration-dependent manner. Induced EZH2 degradation through the UPS. Cell Proliferation Assay[1] Cell Types: BT549, MDA-MB-468, SUM159 and MDA-MB-453 cells Tested Concentrations: 0.1-10 μM Incubation Duration: 5 days Experimental Results: demonstrated superior cellular growth inhibition activity in a panel of TNBC cells. |
| References |
[1]. Brandon Dale, et al. Targeting Triple-Negative Breast Cancer by a Novel Proteolysis Targeting Chimera Degrader of Enhancer of Zeste Homolog 2. ACS Pharmacol Transl Sci. 2022 Jun 24;5(7):491-507.
|
| Molecular Formula |
C65H87N9O8S
|
|---|---|
| Molecular Weight |
1154.51
|
| CAS # |
2855085-25-3
|
| SMILES |
N(C1CCOCC1)(C1C(C)=C(C(=O)NCC2C(=O)NC(C)=CC=2C)C=C(C2C=CC(CN3CCN(C(=O)CCCCCCCC(=O)N[C@@H](C(C)(C)C)C(N4C[C@H](O)C[C@H]4C(=O)NCC4C=CC(C5SC=NC=5C)=CC=4)=O)CC3)=CC=2)C=1)CC
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : 120 mg/mL (103.94 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.25 mg/mL (2.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 32.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8662 mL | 4.3308 mL | 8.6617 mL | |
| 5 mM | 0.1732 mL | 0.8662 mL | 1.7323 mL | |
| 10 mM | 0.0866 mL | 0.4331 mL | 0.8662 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
