Tazemetostat [1403254-99-8]
Referência HY-13803-5mg
Tamanho : 5mg
Marca : MedChemExpress
Tazémétostat (EPZ-6438) est un inhibiteur puissant, sélectif de EZH2 et disponible par voie orale. Tazémétostat (EPZ-6438) inhibe l'activité du complexe répressif humain 2 polycomb (PRC2) contenant du type sauvage EZH2 avec une valeur Ki de 2,5 nM. Tazémétostat (EPZ-6438) inhibe EZH2 avec des IC50 de 11 et 16 nM dans le dosage des peptides et le dosage des nucléosomes, respectivement. Tazémétostat (EPZ-6438) inhibe l'EZH2 de rat avec un IC50 de 4 nM. Tazémétostat (EPZ-6438) inhibe également EZH1 avec un IC50 de 392 nM.
Tazemetostat (EPZ-6438) ist ein wirksamer, selektiver und oral verfügbarer EZH2-Inhibitor. Tazemetostat (EPZ-6438) hemmt die Aktivität des humanen Polycomb-repressiven Komplexes 2 (PRC2), der Wildtyp-EZH2 mit einem Ki-Wert von 2,5 nM enthält. Tazemetostat (EPZ-6438) hemmt EZH2 mit IC50 -Werten von 11 und 16 nM im Peptidassay bzw. im Nucleosomentest. Tazemetostat (EPZ-6438) hemmt Ratten-EZH2 mit einem IC50 von 4 nM. Tazemetostat (EPZ-6438) hemmt auch EZH1 mit einem IC50 von 392 nM.
Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
![Tazemetostat Chemical Structure Tazemetostat Chemical Structure](/proxy_img/Ly9maWxlLm1lZGNoZW1leHByZXNzLmNvbS9wcm9kdWN0X3BpYy9oeS0xMzgwMy5naWY=.gif)
Tazemetostat Chemical Structure
CAS No. : 1403254-99-8
Size | Prix | Stock | Quantité |
---|---|---|---|
Solid + Solvent (Highly Recommended) | |||
10 mM * 1 mL
in DMSO
ready for reconstitution
|
En stock | ||
Solution | |||
10 mM * 1 mL in DMSO | En stock | ||
Solid | |||
5 mg | En stock | ||
10 mg | En stock | ||
50 mg | En stock | ||
100 mg | En stock | ||
200 mg | En stock | ||
500 mg | Obtenir un devis | ||
1 g | Obtenir un devis |
* Veuillez sélectionner la quantité avant d'ajouter des articles.
This product is a controlled substance and not for sale in your territory.
Based on 65 publication(s) in Google Scholar
Other Forms of Tazemetostat:
- Tazemetostat trihydrochloride Obtenir un devis
- Tazemetostat hydrochloride Obtenir un devis
- Tazemetostat hydrobromide Obtenir un devis
- Tazemetostat (Standard) Obtenir un devis
-
Tazemetostat purchased from MedChemExpress. Usage Cited in: Nat Struct Mol Biol. 2018 Mar;25(3):225-232. [Abstract]
- Western blots of extracts from E14 mESCs treated with 10 μM. EPZ6438 EZH2 inhibitor for 7 d and sampled at time points following inhibitor washout. Blots are probed with the indicated antibodies.
-
Tazemetostat purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2018 Jan 2;128(1):483-499. [Abstract]
- Immunoblotting for N1-ICD (n=3) in mouse podocytes exposed to 10 μM EPZ-6438 for 48 hours.
-
Tazemetostat purchased from MedChemExpress. Usage Cited in: Toxins (Basel). 2017 May 16;9(5). pii: E162. [Abstract]
- Cells are treated with LeTx in the presence or absence of GSK-J4 or EPZ-6438 for 48 h. H3K27me3 level is analyzed by Western blotting.
Description |
Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells[1]. |
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
IC50 & Target[1] |
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Cellular Effect |
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
In Vitro |
Tazemetostat (EPZ-6438) inhibits multi wild-type and mutant lymphoma cell lines proliferation with IC50s of 0.49 nM-7.6 μM[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation Assay[1]
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
In Vivo |
Tazemetostat (EPZ-6438; 250 or 500 mg/kg twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Masse moléculaire |
572.74 |
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Formule |
C34H44N4O4 |
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
CAS No. |
1403254-99-8 |
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Appearance |
Solid |
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Color |
White to light yellow |
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
SMILES |
O=C(C1=CC(C2=CC=C(CN3CCOCC3)C=C2)=CC(N(CC)C4CCOCC4)=C1C)NCC5=C(C)C=C(C)NC5=O |
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Livraison | Room temperature in continental US; may vary elsewhere. |
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Stockage |
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Solvant et solubilité |
In Vitro:
DMSO : 31.25 mg/mL (54.56 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) 0.1 M HCL : 14.29 mg/mL (24.95 mM; ultrasonic and adjust pH to 5 with HCl) Preparing
Stock Solutions
View the Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
Tween-80
+
%
Saline
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Pureté et documentation |
Purity: 99.93% |
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Références |
|
Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
---|
0.1 M HCL / DMSO | 1 mM | 1.7460 mL | 8.7300 mL | 17.4599 mL | 43.6498 mL |
5 mM | 0.3492 mL | 1.7460 mL | 3.4920 mL | 8.7300 mL | |
10 mM | 0.1746 mL | 0.8730 mL | 1.7460 mL | 4.3650 mL | |
15 mM | 0.1164 mL | 0.5820 mL | 1.1640 mL | 2.9100 mL | |
20 mM | 0.0873 mL | 0.4365 mL | 0.8730 mL | 2.1825 mL | |
DMSO | 25 mM | 0.0698 mL | 0.3492 mL | 0.6984 mL | 1.7460 mL |
30 mM | 0.0582 mL | 0.2910 mL | 0.5820 mL | 1.4550 mL | |
40 mM | 0.0436 mL | 0.2182 mL | 0.4365 mL | 1.0912 mL | |
50 mM | 0.0349 mL | 0.1746 mL | 0.3492 mL | 0.8730 mL |
Tazemetostat Related Classifications
- Epigenetics Apoptosis
- Histone Methyltransferase Apoptosis
-
Keywords:
Tazemetostat1403254-99-8EPZ-6438 E-7438EPZ6438EPZ 6438E7438E 7438E-7438Histone MethyltransferaseApoptosisEZH2PRC2EZH1epigeneticcancerInhibitorinhibitorinhibit