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Lirametostat (CPI-1205) EZH2 Inhibitor

Name: Lirametostat (CPI-1205)
Brand: Selleck Chemicals
SKU: S8353
Availability: InStock
Rating: 5 (9 reviews)

Cat.No.S8353

Lirametostat (CPI-1205) is an orally available selective inhibitor of the histone lysine methyltransferase EZH2 with IC50 values of 2 nM and 52 nM for EZH2 and EZH1 respectively. It has potential antineoplastic activity.

Chemical Structure

Molecular Weight: 518.57

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Quality Control

Batch: Purity: 99.04%

99.04

Related Targets	PRMT MAT2A DNA Methyltransferase LSD1 JMJD G9a/GLP MLL NSD FTO SETD
Other EZH2 Inhibitors	PF-06821497 GSK126 Tulmimetostat (CPI-0209) Valemetostat (DS-3201) GSK343 CPI-169 SHR2554 EZH2/HSP90-IN-29 EBI-2511

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (192.83 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.64mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	518.57	Formula	C₂₇H₃₃F₃N₄O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1621862-70-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CPI 1205, CPI1205			Smiles	CC1=CC(=C(C(=O)N1)CNC(=O)C2=C(N(C3=CC=CC=C32)C(C)C4CCN(CC4)CC(F)(F)F)C)OC

Mechanism of Action

Targets/IC₅₀/Ki	EZH2 (Cell-free assay) 2 nM EZH1 (Cell-free assay) 52 nM
In vitro	Treatment with Lirametostat (CPI-1205), an EZH2 inhibitor, caused apoptosis in multiple myeloma and plasmacytoma cell models.
In vivo	Lirametostat (CPI-1205) shows excellent oral bioavailability and was well-tolerated for repeat dosing, as demonstrated by the absence of significant body weight loss. It shows relatively high clearance in both rats and dogs (3.19 L/h/kg and 1.41 L/h/kg, respectively) but demonstrates good oral bioavailability in both species (44.6% F in rats and 46.2% F in dogs). This compound was well-tolerated in the 28-day GLP toxicology studies, and any findings were reversible over the recovery period.
References	[1] https://pubmed.ncbi.nlm.nih.gov/27739677/ [2] http://www.bloodjournal.org/content/128/22/5672?sso-checked=true

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02395601	Completed	B-Cell Lymphoma	Constellation Pharmaceuticals	March 2015	Phase 1

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