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EPZ020411 2HCl (1700663-41-7(free base))
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Catalog No. T4334
EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).
EPZ020411 2HCl (1700663-41-7(free base))
😃Good
Catalog No. T4334
EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $108 | Backorder | |
| 5 mg | $192 | Backorder | |
| 10 mg | $306 | Backorder | |
| 25 mg | $639 | Backorder | |
| 1 mL x 10 mM (in DMSO) | $306 | Backorder |
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Product Introduction
Bioactivity
Chemical Properties
| Description | EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM). |
| Targets&IC50 | PRMT8:223 nM, PRMT1:119 nM, PRMT6:10 nM |
| In vitro | In A375 human melanoma cells exogenously overexpressing PRMT6,treatment with EPZ020411IC50=0.637±0.241 μM) results in a dose-dependent decrease in H3R2 methylation. |
| In vivo | Male Sprague-Dawley rats administered a single dose of EPZ020411 (1 mg/kg by i.v.) ,show a moderate clearance (CL) of 19.7±1.0 mL/min/kg, with a volume of distribution at steady state (Vss) of 11.1±1.6 L/kg, translating to a mean terminal half-life (t1/2) of 8.54±1.43 h. At dose of EPZ020411(5 mg/kg s.c.) a good bioavailability of 65.6 ± 4.3% is observed, resulting on EPZ020411 unbound blood concentration remaining above the PRMT6 biochemical IC50 value for more than 12 h. |
| Cell Research | A375 (CRL-1619) cells are incubated in the presence of increasing concentrations of EPZ020411 up to 20 μM for 48 hours. |
| Animal Research | Sprague-Dawley rats are treated with EPZ020411(1 mg/kg i.v.) prepared in saline, pH 6.5. |
| Molecular Weight | 515.51 |
| Formula | C25H40Cl2N4O3 |
| Smiles | Cl.Cl.CNCCN(C)Cc1c[nH]nc1-c1ccc(O[C@H]2C[C@@H](C2)OCCC2CCOCC2)cc1 |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: 93 mg/mL (180.4 mM) DMSO: 93 mg/mL (180.4 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
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