CPI-360

Catalog No.S7656

For research use only.

CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.

CPI-360 Chemical Structure

CAS No. 1802175-06-9

Selleck's CPI-360 has been cited by 1 Publication

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.
Targets
EZH1 [1]
()
102.3 nM
In vitro

In KARPAS-422 cells, CPI-360 potently reduces global H3K27me3 and H3K27me2 levels with EC50 of 56 nM and 65 nM, respectively. CPI-360 also causes time-dependent transcriptional changes, and affects the viability of Y641N mutant EZH2-containing KARPAS-422 cells. In addition, CPI-360 gradually arrests KARPAS-422 cells in the G1 cell cycle stage followed by the induction of apoptosis. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HeLa cells NXTid3VDTnWwY4Tpc44h[XO|YYm= NIDxZ444OiCq NFu2SmZKdmirYnn0bY9vKG:oIFXaTFIhcW5iaIXtZY4hUGWOYTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hUDONMkft[VMhdGW4ZXzzJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IFXMTXNCKG2ndHjv[EwhUUN3ME2wMlA4PSEQvF2= NYnjPWhrOjZzOEmwO|g>
In vivo In mice bearing KARPAS-422 xenografts, CPI-360 (200 mg/kg, s.c.) reduces tumor growth by 44%. [1]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: Mice bearing KARPAS-422 tumors
  • Dosages: 200 mg/kg, twice daily
  • Administration: s.c.

Solubility (25°C)

In vitro

DMSO 20 mg/mL warmed
(45.71 mM)
Ethanol 18 mg/mL warmed
(41.14 mM)
Water Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
10% DMSO+60% PEG 400+ddH2O
For best results, use promptly after mixing.

20mg/mL

Chemical Information

Molecular Weight 437.53
Formula

C25H31N3O4

CAS No. 1802175-06-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=C(C(=O)N1)CNC(=O)C2=C(N(C3=CC=CC=C32)C(C)C4CCOCC4)C)OC

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

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

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