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Tazemetostat hydrobromide

Catalog No. T17002 CAS 1467052-75-0

Synonyms: E-7438 hydrobromide, EPZ-6438 hydrobromide

Tazemetostat hydrobromide (E-7438 hydrobromide) is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 (Ki: 2.5 nM). Tazemetostat hydrobromide also inhibits EZH1 (IC50: 392 nM).

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Tazemetostat hydrobromide Chemical Structure

Tazemetostat hydrobromide, CAS 1467052-75-0

Pack Size	Availability	Price/USD
2 mg	In stock	$ 36.00
5 mg	In stock	$ 55.00
10 mg	In stock	$ 74.00
50 mg	In stock	$ 97.00
100 mg	In stock	$ 162.00
200 mg	In stock	$ 243.00
500 mg	In stock	$ 397.00
1 mL * 10 mM (in DMSO)	In stock	$ 76.00

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Purity: 99.03%

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Description	Tazemetostat hydrobromide (E-7438 hydrobromide) is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 (Ki: 2.5 nM). Tazemetostat hydrobromide also inhibits EZH1 (IC50: 392 nM).
Targets&IC50	EZH2 (rat):4 nM, EZH2:11 nM (in peptide assay), EZH2:16 nM (in nucleosome assay), EZH2 (WT):2.5 nM (Ki), EZH1:392 nM
In vitro	Tazemetostat hydrobromide inhibits Rat EZH2 (IC50: 4 nM). Tazemetostat hydrobromide inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide inhibits multi wild-type and mutant lymphoma cell lines proliferation with IC50s of 0.49 nM-7.6 μM [1].
In vivo	Tazemetostat (250 or 500 mg/kg twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors [1].

Synonyms	E-7438 hydrobromide, EPZ-6438 hydrobromide
Molecular Weight	653.65
Formula	C34H45BrN4O4
CAS No.	1467052-75-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (152.99 mM), Sonification is recommended.

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Inhibitor Library Anti-Cancer Active Compound Library Targeted Therapy Drug Library Epigenetics Compound Library Orally Active Compound Library Anti-Cancer Compound Library Bioactive Compound Library

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Related compounds with same targets

UNC0646 NSD2-IN-4 MS023 EPZ031686 GSK3326595 DCLX069 SGC0946 MI-463

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Tazemetostat hydrobromide 1467052-75-0 Chromatin/Epigenetic Histone Methyltransferase Tazemetostat EPZ 6438 Hydrobromide E 7438 EPZ-6438 Hydrobromide E7438 E-7438 hydrobromide PRC2 Inhibitor E-7438 epigenetic Tazemetostat Hydrobromide EZH2 EPZ6438 EPZ6438 Hydrobromide EPZ-6438 cancer EPZ-6438 hydrobromide E 7438 Hydrobromide E-7438 Hydrobromide E7438 Hydrobromide EPZ 6438 inhibit EZH1 inhibitor

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