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CM272 DNA Methyltransferase inhibitor

Name: CM272
Brand: Selleck Chemicals
SKU: S8812
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S8812

CM-272 is a novel first-in-class dual reversible inhibitor of G9a (GLP) and DNMTs with IC50 of 8 nM, 382 nM, 85 nM, 1200 nM, 2 nM for G9a, DNMT1, DNMT3A, DNMT3B, GLP, respectively. This compound prolongs survival in in vivo models of haematological malignancies by at least in part inducing immunogenic cell death.

Chemical Structure

Molecular Weight: 478.63

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Quality Control

Batch: Purity: 99.89%

99.89

Related Targets	HDAC JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK
Other DNA Methyltransferase Inhibitors	RG108 SGI-1027 Zebularine (NSC 309132) Gamma-Oryzanol GSK3685032 β-thujaplicin GSK-3484862 Bobcat339 DC-05 2'-Deoxy-5-Fluorocytidine

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
CEMO1	Antiproliferative assay	48 hrs	Antiproliferative activity against human CEMO1 cells after 48 hrs by MTS assay, GI50=0.218μM.	29890830
CEMO1	Growth inhibition assay	48 hrs	Growth inhibition of human CEMO1 cells after 48 hrs by MTS assay, GI50=0.218μM.	29953809
MV4-11	Growth inhibition assay	48 hrs	Growth inhibition of human MV4-11 cells after 48 hrs by MTS assay, GI50=0.269μM.	29953809
OCI-LY3	Antiproliferative assay	48 hrs	Antiproliferative activity against human OCI-LY3 cells after 48 hrs by MTS assay, GI50=0.409μM.	29890830
OCI-LY3	Growth inhibition assay	48 hrs	Growth inhibition of human OCI-LY3 cells after 48 hrs by MTS assay, GI50=0.409μM.	29953809
OCI-LY10	Antiproliferative assay	48 hrs	Antiproliferative activity against human OCI-LY10 cells after 48 hrs by MTS assay, GI50=0.455μM.	29890830
OCI-LY10	Growth inhibition assay	48 hrs	Growth inhibition of human OCI-LY10 cells after 48 hrs by MTS assay, GI50=0.455μM.	29953809
LAL-CUN-2	Growth inhibition assay	48 hrs	Growth inhibition of human LAL-CUN-2 cells after 48 hrs by MTS assay, GI50=0.664μM.	29953809
THLE2	Cytotoxicity assay	72 hrs	Cytotoxicity against human THLE2 cells assessed as reduction in cell viability after 72 hrs by MTS assay, LC50=1.78μM.	29890830
THLE2	Growth inhibition assay	72 hrs	Growth inhibition of human THLE2 cells after 72 hrs by MTS assay, LC50=1.78μM.	29953809
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 96 mg/mL (200.57 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 96 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.	4.850mg/ml (10.13mM)	Taking the 1 mL working solution as an example, add 50 μL of 97 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.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.600mg/ml (1.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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	478.63	Formula	C₂₈H₃₈N₄O₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1846570-31-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=CC=C(O1)C2=NC3=CC(=C(C=C3C(=C2)NC4CCN(CC4)C)OC)OCCCN5CCCC5

Mechanism of Action

Targets/IC₅₀/Ki	G9a (Cell-free assay) 8 nM DNMT3A (Cell-free assay) 85 nM DNMT1 (Cell-free assay) 382 nM DNMT3B (Cell-free assay) 1200 nM
In vitro	The GI₅₀ for CM-272 after 48 h of treatment in ALL, AML and DLBCL-derived cell lines is in the nM range and is associated with a decrease in global levels of H3K9me2 and 5mC. This compound inhibits cell proliferation, blocks cell cycle progression and induces apoptosis in ALL, AML and DLBCL cell lines in a dose-dependent manner. It induces IFN response and immunogenic cell death..
In vivo	CM272 therapy induces a statistically significant increase in overall survival (OS) in mice in comparison with control animals. Global H3K9me2 and 5mC levels are reduced in leukaemic cells obtained from mice engrafted with ALL-derived CEMO-1 cells after 1 week of treatment and no significant weight loss is observed in treated animals. This compound shows dose-dependent efficacy and a dose of 2.5 mg/kg of this chemical is adequate to demonstrate the positive anti-tumour efficacy in mice engrafted with ALL-derived CEMO-1 cells..
References	[1] https://pubmed.ncbi.nlm.nih.gov/28548080/

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