Tazemetostat (EPZ-6438)

CAS No.
1403254-99-8
Chemical Name:
Tazemetostat (EPZ-6438)
Synonyms
Tazemetostat;EPZ-6438;E-7438;CS-971;CPDB1064;EPZ-7438;EPZ-6438(E7438);E7438, Tazemetostat;Tazemetostat EPZ-6438;Henagliflozin Proline
CBNumber:
CB82655404
Molecular Formula:
C34H44N4O4
Molecular Weight:
572.74
MDL Number:
MFCD24849415
MOL File:
1403254-99-8.mol
Last updated:2023-11-30 21:41:49

Tazemetostat (EPZ-6438) Properties

Melting point >162°C (dec.)
Boiling point 750.8±60.0 °C(Predicted)
Density 1.163±0.06 g/cm3(Predicted)
storage temp. -20°C
solubility Soluble in DMSO (up to at least 25 mg/ml).
pka 11.92±0.10(Predicted)
form solid
color Off-white
Stability Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
FDA UNII Q40W93WPE1

SAFETY

Risk and Safety Statements

NFPA 704
0
2 0

Tazemetostat (EPZ-6438) price More Price(37)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 16174 EPZ6438 ≥98% 1403254-99-8 1mg $44 2024-03-01 Buy
Cayman Chemical 16174 EPZ6438 ≥98% 1403254-99-8 5mg $130 2024-03-01 Buy
Cayman Chemical 16174 EPZ6438 ≥98% 1403254-99-8 10mg $235 2024-03-01 Buy
Cayman Chemical 16174 EPZ6438 ≥98% 1403254-99-8 50mg $745 2024-03-01 Buy
TRC E592250 EPZ6438 1403254-99-8 1mg $50 2021-12-16 Buy
Product number Packaging Price Buy
16174 1mg $44 Buy
16174 5mg $130 Buy
16174 10mg $235 Buy
16174 50mg $745 Buy
E592250 1mg $50 Buy

Tazemetostat (EPZ-6438) Chemical Properties,Uses,Production

Description

Tazemetostat (1403254-99-8) is a potent (Ki = 2.5nM wild type human PRC2-containing) and selective SAM-competitive inhibitor of the lysine methyltransferase EZH2.1?Tazemetostat displayed strong antiproliferative effects against SMARCB1-deleted malignant rhabdoid tumor (MRT) cell lines?in vitro. This antitumor activity was also observed in SMARTCB1 mutant mouse xenografts. It displayed potent antitumor activity in various cancer models including non-Hodgkins lymphoma2, pediatric glioma3, small-cell carcinoma of the ovary4, and synovial sarcomas5. Tazemetostat has also been shown to control inflammatory genes by modulating IRF1, IRF8, and STAT1 levels suggesting therapeutic potential for the treatment of neuroinflammatory diseases associated with microglial activation.6

Uses

EPZ 6438 is a potent and selective inhibitor of EZH2.

Biological Activity

Tazemetostat (EPZ-6438) is a potent, and selective EZH2 inhibitor with K i and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMT.

target

EZH2(Cell-free assay)

References

1) Knutson?et al.?(2013),?Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2;?Proc. Natl. Acad. Sci. USA?110?7922 2) Knutson?et al.?(2014),?Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma; Mol.Cancer Ther.?13?842 3) Mohammad?et al. (2017),?EZH2 is a potential therapeutic target for H3K27M-mutant pediatric gliomas; Nat. Med.?23?483 4) Chan-Penebre?et al.?(2017),?Selective killing of SMARCA2- and SMARCA4-deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models; Mol. Cancer Ther.?16?850 5) Kawano?et al.?(2016),?Preclinical Evidence of Anti-Tumor Activity by EZH2 Inhibition in Human Models of Synovial Sarcoma; PLoS One?11?e0158888 6) Arifuzzaman?et al.?(2017),?Selective inhibition of EZH2 by a small molecule inhibitor regulates microglial gene expression essential for inflammation; Biochem. Pharmacol.?137?61

Tazemetostat (EPZ-6438) Preparation Products And Raw materials

Raw materials

Preparation Products