EPZ6438 free base · Synonyms: Tazemetostat

Tazemetostat is an orally available, small molecule selective and S-adenosyl methionine competitive inhibitor of histone methyltransferase EZH2.

For research use only. Not for human or veterinary use.

Target Histone Methyltransferase Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

EPZ6438 structure

CAS No.: 1403254-99-8

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
5 g	USD 495.00	BP-02307-5g	In stock	Get quote
10 g	USD 792.00	BP-02307-10g	In stock	Get quote
25 g	USD 1,584.00	—	In stock	Get quote

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Description

Tazemetostat is an orally available, small molecule selective and S-adenosyl methionine (SAM) competitive inhibitor of histone methyltransferase EZH2, with potential antineoplastic activity. Upon oral administration, Tazemetostat selectively inhibits the activity of both wild-type and mutated forms of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 lysine 27 (H3K27).

Biological activity

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.

Identifiers

SMILES: CCN(C1CCOCC1)C1=C(C)C(=CC(=C1)C1=CC=C(CN2CCOCC2)C=C1)C(=O)NCC1=C(C)C=C(C)NC1=O
InChIKey: NSQSAUGJQHDYNO-UHFFFAOYSA-N

Specifications

MW (average): 572.7376
Formula: C₃₄H₄₄N₄O₄
CAS No.: 1403254-99-8
Physical state: Solid
Color: White to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Knutson, Sarah K et al. “Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2.” Proceedings of the National Academy of Sciences of the United States of America vol. 110,19 (2013): 7922-7.

Same target

Search Histone Methyltransferase

Same research area

Search Cancer