Tazemetostat


CAS No. : 1403254-99-8

(Synonyms: EPZ-6438; E-7438)

1403254-99-8
Price and Availability of CAS No. : 1403254-99-8
Size Price Stock
1mg $30 In-stock
5mg $60 In-stock
10mg $84 In-stock
50mg $120 In-stock
100mg $190 In-stock
200mg $290 In-stock
500mg $600 In-stock
1g $960 In-stock
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Cat. No. : HY-13803
M.Wt: 572.74
Formula: C34H44N4O4
Purity: >98 %
Solubility: 0.1 M HCL : 14.29 mg/mL (ultrasonic;adjust pH to 5 with HCl);DMSO : 31.25 mg/mL (ultrasonic;warming;heat to 60°C)
Introduction of 1403254-99-8 :

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:Ki: 2.5 nM (EZH2)[1] 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]. In Vivo:Tazemetostat (EPZ-6438; 250 or 500 mg/kg twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors[1].

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