Art. -Nr.: HY-101925

CM-272

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC₅₀s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death.

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Reinheit: 99.55%
CAS. Nr.: 1846570-31-7
Formel: C₂₈H₃₈N₄O₃
Molecular Weight:478.63

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CM-272 Chemical Structure

CAS. Nr.: 1846570-31-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

G9a

8 nM (IC₅₀)

EHMT1/GLP/KMT1D

2 nM (IC₅₀)

DNMT1

382 nM (IC₅₀)

DNMT3A

85 nM (IC₅₀)

DNMT3B

1200 nM (IC₅₀)

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Alle DNA Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF-10A	EC₅₀	0.2 μM Compound: 2;CM-272	Antitumor activity against human spontaneously immortalized CDH-/- MCF10A cells assessed as cell numbers measured after 48 hrs Antitumor activity against human spontaneously immortalized CDH-/- MCF10A cells assessed as cell numbers measured after 48 hrs	[PMID: 34878770]
MCF-10A	EC₅₀	0.5 μM Compound: 2;CM-272	Antitumor activity against human spontaneously immortalized wild type MCF-10A cells assessed as cell numbers measured after 48 hrs Antitumor activity against human spontaneously immortalized wild type MCF-10A cells assessed as cell numbers measured after 48 hrs	[PMID: 34878770]
MM1.S	GI₅₀	1041 nM Compound: 5; CM-272	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation measured up to 72 hrs by CellTiter96 Aqueous one reagent based assay Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation measured up to 72 hrs by CellTiter96 Aqueous one reagent based assay	[PMID: 33661013]
MV4-11	GI₅₀	269 nM Compound: 12; CM-272	Growth inhibition of human MV4-11 cells after 48 hrs by MTS assay Growth inhibition of human MV4-11 cells after 48 hrs by MTS assay	[PMID: 29953809]
OCI-Ly10	GI₅₀	455 nM Compound: 12; CM-272	Growth inhibition of human OCI-LY10 cells after 48 hrs by MTS assay Growth inhibition of human OCI-LY10 cells after 48 hrs by MTS assay	[PMID: 29953809]
OCI-Ly10	GI₅₀	455 nM Compound: 5	Antiproliferative activity against human OCI-LY10 cells after 48 hrs by MTS assay Antiproliferative activity against human OCI-LY10 cells after 48 hrs by MTS assay	[PMID: 29890830]
OCI-Ly3	GI₅₀	409 nM Compound: 12; CM-272	Growth inhibition of human OCI-LY3 cells after 48 hrs by MTS assay Growth inhibition of human OCI-LY3 cells after 48 hrs by MTS assay	[PMID: 29953809]
OCI-Ly3	GI₅₀	409 nM Compound: 5	Antiproliferative activity against human OCI-LY3 cells after 48 hrs by MTS assay Antiproliferative activity against human OCI-LY3 cells after 48 hrs by MTS assay	[PMID: 29890830]

In Vitro

CM-272 (100-1000 nM; 12-72 hours; CEMO-1, MV4-11 and OCI-Ly10 cell lines) treatment inhibits cell proliferation in a dose- and time-dependent manner^[1].
CM-272 (100-1000 nM; 24 hours; CEMO-1, MV4-11 and OCI-Ly10 cell lines) treatment blocks cell cycle progression^[1].
CM-272 (100-1000 nM; 12-72 hours; CEMO-1, MV4-11, and OCI-Ly10 cell lines) treatment induces apoptosis in ALL, AML and DLBCL cell lines in a dose- and time-dependent manner^[1].
CM-272 after 48 h of treatment CEMO-1 acute lymphoblastic leukaemia (ALL) cell line, MV4-11 acute myeloid leukaemia (AML) cell line, and OCI-Ly10 diffuse large B-cell lymphoma (DLBCL) cell line, the GI₅₀ values of 218 nM, 269 nM and 455 nM, respectively, and is associated with a decrease in global levels of H3K9me2 and 5mC^[1].
The therapeutic activity of CM-272 relies on the early activation of the type I IFN response in tumor cells, potentially leading to the induction of cell-autonomous immunogenic death in tumor cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

CEMO-1, MV4-11 and OCI-Ly10 cell lines
Concentration:

125 nM, 250 nM, 500 nM (CEMO-1 cells); 135 nM, 270 nM, 540 nM (MV4-11 cells); 100 nM, 400 nM, 1000 nM (OCI-Ly10 cells)
Incubation Time:

12 hours, 24 hours, 48 hours and 72 hours
Result:

Inhibited cell proliferation in a dose- and time-dependent manner.

Cell Cycle Analysis^[1]

Cell Line:

CEMO-1, MV4-11 and OCI-Ly10 cell lines
Concentration:

125 nM, 250 nM, 500 nM (CEMO-1 cells); 135 nM, 270 nM, 540 nM (MV4-11 cells); 100 nM, 400 nM, 1000 nM (OCI-Ly10 cells)
Incubation Time:

24 hours
Result:

Blocked cell cycle progression.

Apoptosis Analysis^[1]

Cell Line:

CEMO-1, MV4-11 and OCI-Ly10 cell lines
Concentration:

125 nM, 250 nM, 500 nM (CEMO-1 cells); 135 nM, 270 nM, 540 nM (MV4-11 cells); 100 nM, 400 nM, 1000 nM (OCI-Ly10 cells)
Incubation Time:

12 hours, 24 hours, 48 hours and 72 hours
Result:

Induced apoptosis in ALL, AML and DLBCL cell lines in a dose- and time-dependent manner.

In Vivo

CM-272 (2.5 mg/kg; intravenous injection; daily; for 28 days; female Rag2^/γc^/ mice) treatment significantly prolongs survival of CEMO-1 cells xenogeneic models^[1].

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

Animal Model:

Female BALB/Ca-Rag2^−/−γc^−/− mice (6–8-week-old) with CEMO-1 cells^[1]
Dosage:

2.5 mg/kg
Administration:

Intravenous injection; daily; for 28 days
Result:

Induced a statistically significant increase in overall survival (OS) in mice.

Chemical Information

CAS. Nr. 1846570-31-7
Appearance Solid
Molecular Weight 478.63
Formel C₂₈H₃₈N₄O₃
Color Off-white to light yellow
SMILES

CN(CC1)CCC1NC2=CC(C3=CC=C(C)O3)=NC4=CC(OCCCN5CCCC5)=C(OC)C=C42
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (3)

All

Sort by:

Journal Impact Factor

Adv Mater

Unzippable Siamese Nanoparticles for Programmed Two-Stage Cancer Immunotherapy. [Abstract]

2024 Aug;36(31):e2402456. PMID: 38810924
Biochim Biophys Acta Gen Subj

G9a and DNMT1 inhibition modulates CDKN1A promoter methylation and the cell cycle leading to improvement in kidney fibrosis. [Abstract]

2023 Sep;1867(9):130417. PMID: 37356504
University of California

2024.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (261.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0893 mL

10.4465 mL

20.8930 mL

5 mM

0.4179 mL

2.0893 mL

4.1786 mL

10 mM

0.2089 mL

1.0446 mL

2.0893 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

Solubility: ≥ 2.08 mg/mL (4.35 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. San José-Enériz E, et al. Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies. Nat Commun. 2017 May 26;8:15424. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0893 mL	10.4465 mL	20.8930 mL	52.2324 mL
	5 mM	0.4179 mL	2.0893 mL	4.1786 mL	10.4465 mL
	10 mM	0.2089 mL	1.0446 mL	2.0893 mL	5.2232 mL
	15 mM	0.1393 mL	0.6964 mL	1.3929 mL	3.4822 mL
	20 mM	0.1045 mL	0.5223 mL	1.0446 mL	2.6116 mL
	25 mM	0.0836 mL	0.4179 mL	0.8357 mL	2.0893 mL
	30 mM	0.0696 mL	0.3482 mL	0.6964 mL	1.7411 mL
	40 mM	0.0522 mL	0.2612 mL	0.5223 mL	1.3058 mL
	50 mM	0.0418 mL	0.2089 mL	0.4179 mL	1.0446 mL
	60 mM	0.0348 mL	0.1741 mL	0.3482 mL	0.8705 mL
	80 mM	0.0261 mL	0.1306 mL	0.2612 mL	0.6529 mL
	100 mM	0.0209 mL	0.1045 mL	0.2089 mL	0.5223 mL

CM-272

3 Cited Publications

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CM-272

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) CM-272

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Alle DNA Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CM-272

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) CM-272

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Alle DNA Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CM-272 Related Classifications

HY-101925 Related Classifications