| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
|
EPZ011989 TFA is the trifluoroactic acid salt of EPZ-011989, which is an orally bioavailable EZH2 inhibitor with high anticancer activity. It has therapeutic potential for the treatment of B cell lymphomas and other cancer indications.
| ln Vitro |
EPZ-011989 trifluoroacetate inhibits both wild-type and mutant EZH2 with a Ki value of less than 3 nM[1]. EPZ-011989 trifluoroacetate has an IC50 value of 94 nM, which means it can lower cellular H3K27 methylation[1]. WSU-DLCL2 cells are resistant to proliferation when exposed to EPZ-011989 trifluoroacetate (0–10 μM; 11 days) [1].
|
|---|---|
| ln Vivo |
Trifluoroacetate EPZ-011989 (oral; 30-1000 mg/kg; once or twice daily; for 7 or 21 days) causes strong anti-tumor action and methyl tag inhibition [1].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: WSU-DLCL2 Cell Tested Concentrations: 0-10 μM Incubation Duration: 11 days Experimental Results: The average minimum cytotoxic concentration (LCC) in WSU-DLCL2 cells was 208 nM. |
| Animal Protocol |
Animal/Disease Models: SCID (severe combined immunodeficient) mouse [1]
Doses: 125, 250, 500, and 1000 mg/kg Route of Administration: Oral; single dose twice (two times) daily (BID) for 7 days or twice (two times) daily (BID) for 21 days Experimental Results: LCC coverage was provided for 24 hrs (hrs (hours)) (1000 mg/kg), while the 250 and 500 mg/kg doses provided 24 hrs (hrs (hours)) (1000 mg/kg) coverage for approximately 8 hrs (hrs (hours)). Complete ablation of the methyl label was observed at the end of day 7. Demonstrated potent tumor growth inhibition, diminished methyl labelling, and prolonged total and free plasma exposure. Animal/Disease Models: Rat[1] Doses: 30, 100 and 300 mg/kg Route of Administration: po (po (oral gavage)) Single Experimental Results:Dose (mg/kg) Route t1/2 (h) tmax (h) Cmax (ng/mL ) AUCinf (h*ng/mL) Time above LCC (h) 30 po 4.7 2 240 970 4 100 po 3.9 2.7 1600 5600 8 300 po 3.7 2.7 2900 10000 10 |
| References |
| Molecular Formula |
C39H53F6N5O8
|
|---|---|
| Molecular Weight |
833.87
|
| Exact Mass |
719.386
|
| CAS # |
1598383-41-5
|
| Related CAS # |
EPZ011989;1598383-40-4;EPZ011989 hydrochloride;2095432-26-9
|
| PubChem CID |
118704752
|
| Appearance |
Light yellow to yellow solid powder
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
51
|
| Complexity |
1190
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
JAUQBEFSKUVFDO-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C35H51N5O4.C2HF3O2/c1-7-40(30-12-10-29(11-13-30)38(5)15-18-43-6)33-23-28(9-8-14-39-16-19-44-20-17-39)22-31(27(33)4)34(41)36-24-32-25(2)21-26(3)37-35(32)42;3-2(4,5)1(6)7/h21-23,29-30H,7,10-20,24H2,1-6H3,(H,36,41)(H,37,42);(H,6,7)
|
| Chemical Name |
N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl-[4-[2-methoxyethyl(methyl)amino]cyclohexyl]amino]-2-methyl-5-(3-morpholin-4-ylprop-1-ynyl)benzamide;2,2,2-trifluoroacetic acid
|
| Synonyms |
EPZ 011989 TFA EPZ011989 TFA EPZ011989 TFA salt
|
| 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 : ~100 mg/mL (~138.92 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.47 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1992 mL | 5.9961 mL | 11.9923 mL | |
| 5 mM | 0.2398 mL | 1.1992 mL | 2.3985 mL | |
| 10 mM | 0.1199 mL | 0.5996 mL | 1.1992 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
