Product Name :
Tazemetostat trihydrochloride
Description:
Tazemetostat trihydrochloride (EPZ-6438 trihydrochloride) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat trihydrochloride inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki of 2.5 nM. Tazemetostat trihydrochloride inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat trihydrochloride inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM.
CAS:
1403255-00-4
Molecular Weight:
682.12
Formula:
C34H47Cl3N4O4
Chemical Name:
N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-5-[ethyl(oxan-4-yl)amino]-4-methyl-4′-[(morpholin-4-yl)methyl]-[1,1′-biphenyl]-3-carboxamide; tris(chlorohydrogen)
Smiles :
Cl.Cl.Cl.CCN(C1CCOCC1)C1C=C(C=C(C(=O)NCC2C(=O)NC(C)=CC=2C)C=1C)C1=CC=C(CN2CCOCC2)C=C1
InChiKey:
PBAHJOUNGPCAIP-UHFFFAOYSA-N
InChi :
InChI=1S/C34H44N4O4.3ClH/c1-5-38(29-10-14-41-15-11-29)32-20-28(27-8-6-26(7-9-27)22-37-12-16-42-17-13-37)19-30(25(32)4)33(39)35-21-31-23(2)18-24(3)36-34(31)40;;;/h6-9,18-20,29H,5,10-17,21-22H2,1-4H3,(H,35,39)(H,36,40);3*1H
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
Tazemetostat trihydrochloride (EPZ-6438 trihydrochloride) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat trihydrochloride inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki of 2.5 nM. Tazemetostat trihydrochloride inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat trihydrochloride inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM.|Product information|CAS Number: 1403255-00-4|Molecular Weight: 682.12|Formula: C34H47Cl3N4O4|Chemical Name: N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-5-[ethyl(oxan-4-yl)amino]-4-methyl-4′-[(morpholin-4-yl)methyl]-[1,1′-biphenyl]-3-carboxamide; tris(chlorohydrogen)|Smiles: Cl.{{Simtuzumab} web|{Simtuzumab} Monoamine Oxidase|{Simtuzumab} Biological Activity|{Simtuzumab} In Vitro|{Simtuzumab} custom synthesis|{Simtuzumab} Cancer} Cl.{{Escitalopram} web|{Escitalopram} Neuronal Signaling|{Escitalopram} Biological Activity|{Escitalopram} Description|{Escitalopram} custom synthesis|{Escitalopram} Cancer} Cl.PMID:32926338 CCN(C1CCOCC1)C1C=C(C=C(C(=O)NCC2C(=O)NC(C)=CC=2C)C=1C)C1=CC=C(CN2CCOCC2)C=C1|InChiKey: PBAHJOUNGPCAIP-UHFFFAOYSA-N|InChi: InChI=1S/C34H44N4O4.3ClH/c1-5-38(29-10-14-41-15-11-29)32-20-28(27-8-6-26(7-9-27)22-37-12-16-42-17-13-37)19-30(25(32)4)33(39)35-21-31-23(2)18-24(3)36-34(31)40;;;/h6-9,18-20,29H,5,10-17,21-22H2,1-4H3,(H,35,39)(H,36,40);3*1H|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|Tazemetostat (EPZ-6438) inhibits multi wild-type and mutant lymphoma cell lines proliferation with IC50s of 0.49 nM-7.6 μM.|In Vivo:|Tazemetostat (EPZ-6438; 250 or 500 mg/kg twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors.|Products are for research use only. Not for human use.|