EPZ5676

Description

Biological Activity

Protocol(Only for Reference)

Clinical Trial Information( data from http://clinicaltrials.gov)

Chemical Information

References

Name: EPZ5676
Brand: Selleckchem
SKU: S7062

貨號 Cat. No.: S7062
規格 Size: 10mgã€50mg
品牌 Brand: Selleckchem

EPZ5676

Catalog No.S7062

EPZ-5676 is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with K_i of 80 pM, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor. Phase 1.

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10mg	USD 340	In stock	0 1 2 3 4 5 6 7 8 9 10
50mg	USD 1222	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT01684150	Recruiting	Acute Myeloid Leukemia\|Acute Lymphoblastic Leukemia\|Myelodysplastic Syndrome\|Myeloproliferative Disorders\|Chronic Myeloid Leukemia	Epizyme, Inc.\|Celgene Corporation	2012-09	Phase 1

Description

EPZ-5676 is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with K_iof 80 pM, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor. Phase 1.

80 pM K_i

In vitro

EPZ-5676 reduces H3K79 dimethylation with a cellular IC50 of 2.6 nM in MV4-11 cells. EPZ-5676 treatment results in concentration- and time-dependent reduction of H3K79 methylation without effect on the methylation status of other histone sites, which leads to inhibition of key MLL target genes and selective, apoptotic cell killing in MLL-rearranged leukemia cells. EPZ-5676 inhibits proliferation of MLL-AF4 rearranged cell line MV4-11 with an IC50 of 9 nM.

EPZ-5676 continuously intravenous infusion for 21 days to xenograft model of MLL-rearranged leukemia, leads to dose-dependent anti-tumor activity. At the highest dose of 70.5 mg/kg/day, complete tumor regressions are achieved with no regrowth for up to 32 days after the cessation of treatment. No significant weight loss or obvious toxicity is observed in rats treated with EPZ-5676 during efficacy study.

Molecular Weight (MW)	562.71
Formula	C₃₀H₄₂N₈O₃
CAS No.	1380288-87-8

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	N/A

Solubility (25°C) *	In vitro	DMSO	100 mg/mL (177 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	100 mg/mL (177 mM)
	In vivo	30% PEG400/0.5% Tween80/5% propylene glycol,	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	9H-Purin-6-amine, 9-[5-deoxy-5-[[cis-3-[2-[6-(1,1-dimethylethyl)-1H-benzimidazol-2-yl]ethyl]cyclobutyl](1-methylethyl)amino]-β-D-ribofuranosyl]-