EPZ5676

EPZ5676

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Biological Activity

Protocol(Only for Reference)

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

Chemical Information

Preparing Stock Solutions

Research Area

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Choose Your Country or Region

Biological Activity

Protocol(Only for Reference)

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

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In 2013, 835 articles cited Selleck products, including the listed 11 with IF>30.

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In 2013, 835 articles cited Selleck products, including the listed 11 with IF>30.

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Inhibitory Selectivity
Solubility

Cat.No.	Product Name	Solubility (25°C)
Cat.No.	Product Name	Water	DMSO	Ethanol
S8006	BIX 01294	98 mg/mL	98 mg/mL	8 mg/mL
S7004	EPZ005687	<1 mg/mL	2 mg/mL	<1 mg/mL
S7062	EPZ5676	<1 mg/mL	100 mg/mL	100 mg/mL
S7079	SGC 0946	<1 mg/mL	100 mg/mL	100 mg/mL
S3147	Entacapone	<1 mg/mL	61 mg/mL	2 mg/mL
S7120	3-Deazaneplanocin A (DZNeP)	52 mg/mL	52 mg/mL	<1 mg/mL
S7353	EPZ004777	100 mg/mL	100 mg/mL	100 mg/mL
S7128	EPZ-6438	<1 mg/mL	29 mg/mL	<1 mg/mL
S7164	GSK343	<1 mg/mL	1 mg/mL	4 mg/mL
S7165	UNC1999	<1 mg/mL	100 mg/mL	100 mg/mL
S7265	MM-102	100 mg/mL	100 mg/mL	100 mg/mL

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Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Biological Activity Protocol Clinical Trial Information Chemical Information Tech Support & FAQs

1

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

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

Storage	3 years -20℃Powder
Storage	6 months-80℃in 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]-

Stock Solution (1ml DMSO)	1mM	10mM	20mM	30mM
Mass(mg)	0.56271	5.6271	11.2542	16.8813

Molarity Calculator Dilution Calculator Molecular Weight Calculator

AP26113
AP26113 is a potent ALK inhibitor with IC50 of 0.62 nM, demonstrated ability overcome Crizotinib resistance mediated by a L1196M mutation. Phase 1/2.

Features:At least 10-fold more potent and selective in ALK inhibition relative to crizotinib.
EPZ005687
EPZ005687 is a potent and selective inhibitor of EZH2 with K_i of 24 nM, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
VX-680 (Tozasertib, MK-0457)
VX-680 (Tozasertib, MK-0457) is a pan-Aurora inhibitor, mostly against Aurora A with K_i^app of 0.6 nM, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. Phase 2.
Alectinib (CH5424802)
CH5424802 is a potent ALK inhibitor with IC50 of 1.9 nM, sensitive to L1196M mutation and higher selectivity for ALK than PF-02341066, NVP-TAE684 and PHA-E429. Phase 1/2.
LDK378
LDK378 is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. Phase 2.

Features:Does not cross react with c-Met, and has an improved in vivo glucose homeostasis profile relative to TAE684. May be active in Crizotinib-relapsed tumors.
Trametinib (GSK1120212)
Trametinib (GSK1120212) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2. Phase 3.

Features:More potent than PD0325901 or AZD6244.

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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EPZ5676
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.
EPZ005687
EPZ005687 is a potent and selective inhibitor of EZH2 with K_i of 24 nM, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
BIX 01294
BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases.
Entacapone
Entacapone inhibits catechol-O-methyltransferase(COMT) with IC50 of 151 nM.
Decitabine
Decitabine is a potent inhibitor of DNA methylation with IC50 of 438 nM and 4.38 nM in HL-60 and KG1a cells, respectively.
Azacitidine
Azacitidine is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases.
I-BET151 (GSK1210151A)
I-BET151 (GSK1210151A) is a novel selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM, respectively.

Features:Optimized to retain excellent BET target potency and selectivity while enhancing the in vivo pharmacokinetics and terminal half-life to enable prolonged in vivo studies.
RG108
RG108 is an inhibitor of DNA methyltransferase with IC50 of 115 nM, does not cause trapping of covalent enzymes.
PFI-1 (PF-06405761)
PFI-1 is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM.
Thioguanine
Thioguanine is a purine antimetabolite widely used in the treatment of acute lymphoblastic leukemia, autoimmune disorders (e.g., Crohn's disease, rheumatoid arthritis) and organ transplant recipients.

Description

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.

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.