Tazemetostat hydrobromide |
| Catalog No.GC38163 |
Tazemetostat 하이드로브로마이드(EPZ-6438 하이드로브로마이드)는 강력하고 선택적인 경구용 EZH2 억제제입니다. Tazemetostat hydrobromide는 2.5nM의 Ki 값으로 인간 폴리콤 억제 복합체 2(PRC2) 함유 야생형 EZH2의 활성을 억제합니다. Tazemetostat Hydrobromide는 펩타이드 분석과 뉴클레오솜 분석에서 각각 11 및 16 nM의 IC50으로 EZH2를 억제합니다. Tazemetostat Hydrobromide는 4 nM의 IC50으로 쥐 EZH2를 억제합니다. Tazemetostat Hydrobromide는 또한 392nM의 IC50으로 EZH1을 억제합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1467052-75-0
Sample solution is provided at 25 µL, 10mM.
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Tazemetostat hydrobromide (EPZ-6438 hydrobromide) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat hydrobromide inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide inhibits Rat EZH2 with an IC50 of 4 nM. Tazemetostat hydrobromide also inhibits EZH1 with an IC50 of 392 nM.
Tazemetostat (EPZ-6438) inhibits multi wild-type and mutant lymphoma cell lines proliferation with IC50s of 0.49 nM-7.6 μM[1]. Cell Proliferation Assay[1] Cell Line: Wild-type and mutant lymphoma cell lines: DOHH-2 cell (EZH2 wild-type), Farage cell (EZH2 wild-type), OCI-LY19 cell (EZH2 wild-type), Toledo cell (EZH2 wild-type), KARPAS-422 (EZH2 Y646N), Pfeiffer (EZH2 A682G), RL cell line (EZH2 Y646N), SU-DHL-10 (EZH2 Y646F), SU-DHL-6 (EZH2 Y646N), WSU-DLCL2 (EZH2 Y646F)
Tazemetostat (EPZ-6438; 250 or 500 mg/kg twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors[1]. Animal Model: SCID mice bearing s.c. G401 xenografts [1]
[1]. Knutson SK, et al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferaseEZH2. Proc Natl Acad Sci U S A. 2013 May 7;110(19):7922-7.
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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