[CAS NO. 1598383-41-5] EPZ011989trifluoroacetate

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PRODUCTS SPECIFICATIONS [1598383-41-5]

Catalog

HY-16986A

Brand

MCE

CAS

1598383-41-5

DESCRIPTION [1598383-41-5]

Overview

MDL	-
Molecular Weight	719.83
Molecular Formula	C37H52F3N5O6
SMILES	O=C(NCC1=C(C)C=C(C)NC1=O)C2=CC(C#CCN3CCOCC3)=CC(N(CC)[C@H]4CC[C@H](N(CCOC)C)CC4)=C2C.O=C(O)C(F)(F)F

For research use only. We do not sell to patients.

2 Publications Citing Use of MCE

Summary

EPZ-011989 trifluoroacetate is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ-011989 trifluoroacetate has inhibitory inhibition for EZH2 with a K _i value of <3 nM. EPZ-011989 trifluoroacetate shows robust methyl mark inhibition and anti-tumor activity. EPZ-011989 trifluoroacetate can be used for the research of various cancers ^[1] .

IC50 & Target

EZH2

In Vitro

EPZ-011989 trifluoroacetate inhibits mutant and wild-type EZH2 with an K _i value of <3 nM ^[1] .
EPZ-011989 trifluoroacetate reduces cellular H3K27 methylation with an IC ₅₀ value of 94 nM ^[1] .
EPZ-011989 trifluoroacetate (0-10 μM; 11 days) has anti-proliferation effect in WSU-DLCL2 cells ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay ^[1]

Cell Line:	WSU-DLCL2 cells
Concentration:	0-10 μM
Incubation Time:	11 days
Result:	Demonstrated an average lowest cytotoxic concentration (LCC) in WSU-DLCL2 cells of 208 nM.

In Vivo

EPZ-011989 trifluoroacetate (oral; 30-1000 mg/kg; single or bid; for 7 days or 21 days) can elicit robust methyl mark inhibition and antitumor activity ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	SCID mice ^[1]
Dosage:	125, 250, 500, and 1000 mg/kg
Administration:	Oral; single, twice-daily (BID)for 7 days or twice-daily (BID)for 21 days
Result:	Provided coverage over the LCC for 24 h (1000 mg/kg ), while the 250 and 500 mg/kg doses provided coverage over this value for approximately 8 h. Observed complete ablation of the methyl mark by the end of day 7. Showed robust tumor growth inhibition, methyl mark reduction and extended total and free plasma exposure time.

Animal Model:

Rat ^[1]

Dosage:

30, 100, and 300 mg/kg

Administration:

Oral, single

Result:

dose (mg/kg)	route	t _1/2 (h)	t _max (h)	C _max (ng/mL)	AUC _inf (h*ng/mL)	time above LCC (h)
30	p.o.	4.7	2	240	970	4
100	p.o.	3.9	2.7	1600	5600	8
300	p.o.	3.7	2.7	2900	10000	10

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 138.92 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.3892 mL	6.9461 mL	13.8922 mL
5 mM	0.2778 mL	1.3892 mL	2.7784 mL
10 mM	0.1389 mL	0.6946 mL	1.3892 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (3.47 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (3.47 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (3.47 mM); Clear solution

* All of the co-solvents are available by MCE.

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.