EPZ 015666

Name: EPZ 015666
Brand: Tocris Bioscience
SKU: 6516

Tocris Bioscience, part of Bio-Techne | Catalog # 6516

Citations (3)

COA / SDS

Potent and selective PRMT5 inhibitor

Key Product Details

Description:	Potent and selective PRMT5 inhibitor
Chemical Name:	N-[(2S)-3-(3,4-Dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-6-(3-oxetanylamino)-4-pyrimidinecarboxamide
Purity:	≥98% (HPLC)
Molecular Weight:	383.44

View Full Technical Details for EPZ 015666

Technical Data
Citations

Biological Activity for EPZ 015666

EPZ 015666 is a potent and selective protein arginine methyltransferase 5 (PRMT5) inhibitor (IC₅₀ = 22 nM, K_i = 5 nM). Displays selectivity for PRMT5 over a panel of 20 other protein methyltransferases. Exhibits dose-dependent antitumor effects in multiple mantle cell lymphoma (MCL) xenograft models. Orally bioavailable.

Compound Libraries for EPZ 015666

EPZ 015666 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for EPZ 015666

M. Wt	383.44
Formula	C₂₀H₂₅N₅O₃
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1616391-65-1
PubChem ID	90241673
InChi Key	ZKXZLIFRWWKZRY-KRWDZBQOSA-N
Smiles	O[C@H](CN1CCC2=CC=CC=C2C1)CNC(C3=NC=NC(NC4COC4)=C3)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for EPZ 015666

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	38.34	100
	ethanol	19.17	50

Preparing Stock Solutions for EPZ 015666

The following data is based on the product molecular weight 383.44.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.61 mL	13.04 mL	26.08 mL
5 mM	0.52 mL	2.61 mL	5.22 mL
10 mM	0.26 mL	1.30 mL	2.61 mL
50 mM	0.05 mL	0.26 mL	0.52 mL

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References for EPZ 015666

References are publications that support the biological activity of the product.

Chan-Penebre A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models. Nat.Chem.Biol. 2015 PMID: 25915199
Duncan Structure and property guided design in the identification of PRMT5 tool compound EPZ015666. ACS Med.Chem.Lett. 2015 PMID: 26985292