EPZ011989 free base · Synonyms: EPZ-011989 · EPZ 011989

EPZ011989 is a potent and orally active Zeste Homolog 2 inhibitor.

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

Target Histone Methyltransferase

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

EPZ011989 structure

CAS No.: 1598383-40-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 785.00	BP-02335-250mg	In stock	Get quote
500 mg	USD 1,250.00	BP-02335-500mg	In stock	Get quote
1 g	USD 1,800.00	BP-02335-1g	In stock	Get quote
2 g	USD 3,200.00	BP-02335-2g	In stock	Get quote
5 g	Inquire	BP-02335-5g	In stock	Inquire

Need another size or custom synthesis? Request a quote.

Description

EPZ011989 is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ011989 has inhibitory inhibition for EZH2 with a Ki value of <3 nM.

Biological activity

EPZ011989 is also a specific EZH2 inhibitor with a >15-fold selectivity over EZH1 and >3000-fold selectivity relative to the Ki of 20 other histone methyltransferases (HMTs) tested. EPZ011989 reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with an IC50 below 100 nM. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.

Identifiers

SMILES: CCN([C@H]1CC[C@@H](CC1)N(C)CCOC)C1=C(C)C(=CC(=C1)C#CCN1CCOCC1)C(=O)NCC1=C(C)C=C(C)NC1=O
InChIKey: XQFINGFCBFHOPE-WXUXXXNLSA-N

Specifications

MW (average): 605.8105
Formula: C₃₅H₅₁N₅O₄
CAS No.: 1598383-40-4
Physical state: Solid
Color: Light yellow to 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]. Campbell JE, et al. EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity. ACS Med Chem Lett. 2015 Mar 4;6(5):491-495.

Same target

Search Histone Methyltransferase

Same research area

Search Cancer