CM-272
- CAS No.
- 1846570-31-7
- Chemical Name:
- CM-272
- Synonyms
- CM-272;CM-272, 10 mM in DMSO;CM-272; CM 272; CM272;6-Methoxy-2-(5-methylfuran-2-yl)-N-(1-methylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinolin-4-amine;4-Quinolinamine, 6-methoxy-2-(5-methyl-2-furanyl)-N-(1-methyl-4-piperidinyl)-7-[3-(1-pyrrolidinyl)propoxy]-;DNMT1,anti-tumour,DNMTs,immunogenic,DNA MTases,CM272,DNMT3A,CM 272,G9a,H3K9me2,Inhibitor,epigenetics,Histone Methyltransferase,GLP,Apoptosis,inhibit,substrate-competitive,CM-272,DNMT3B,DNA Methyltransferase
- CBNumber:
- CB14632529
- Molecular Formula:
- C28H38N4O3
- Molecular Weight:
- 478.63
- MDL Number:
- MFCD31812316
- MOL File:
- 1846570-31-7.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Boiling point | 631.9±55.0 °C(Predicted) |
|---|---|
| Density | 1.164±0.06 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility |
DMSO:84.0(Max Conc. mg/mL);179.5(Max Conc. mM) Ethanol:63.0(Max Conc. mg/mL);131.63(Max Conc. mM) |
| form | A crystalline solid |
| pka | 10.09±0.20(Predicted) |
| color | Light brown to brown |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P280-P301+P312-P302+P352-P305+P351+P338 |
CM-272 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 25948 | CM-272 ≥95% | 1846570-31-7 | 1mg | $90 | 2026-04-30 | Buy |
| Cayman Chemical | 25948 | CM-272 ≥95% | 1846570-31-7 | 5mg | $197 | 2026-04-30 | Buy |
| Cayman Chemical | 25948 | CM-272 ≥95% | 1846570-31-7 | 10mg | $349 | 2026-04-30 | Buy |
| Cayman Chemical | 25948 | CM-272 ≥95% | 1846570-31-7 | 25mg | $762 | 2026-04-30 | Buy |
| Biosynth | WYC57031 | CM-272 | 1846570-31-7 | 25mg | $1215.75 | 2026-06-05 | Buy |
CM-272 Chemical Properties, Uses, Production
Uses
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[1].
Biological Activity
CM272 is a novel, first-in-class dual reversible inhibitor of G9a (GLP) and DNMTs with IC50 values of 8 nM, 382 nM, 85 nM, 1200 nM, and 2 nM for G9a, DNMT1, DNMT3A, DNMT3B, and GLP, respectively. CM272 prolongs survival in in vivo models of hematological malignancies by at least partially inducing immunogenic cell death.
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.
CM-272 (100-1000 nM; 24 hours; CEMO-1, MV4-11 and OCI-Ly10 cell lines) treatment blocks cell cycle progression.
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.
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 GI 50 values of 218 nM, 269 nM and 455 nM, respectively, and is associated with a decrease in global levels of H3K9me2 and 5mC.
The therapeutic activity of CM-272 relies on the early activation of the type I IFN response in tumour cells , potentially leading to the induction of cell autonomous immunogenic death in tumou r cells.
Cell Proliferation Assay
| 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
| Cell Line: | CEMO-1, MV4-11 and OCI-Ly10 cell lines |
| Concentration: | |
| 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
| 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-dep endent manner. |
in vivo
CM-272 (2.5 mg/kg; injection; daily; for 28 days; female Rag2 intravenous / γc / mice) treatment significantly prolongs survival of CEMO-1 cells xenogeneic models.
| Animal Model: | Female BALB/Ca-Rag2 / γc / mice (6–8-week-old) with CEMO-1 cells |
| Dosage: | 2.5 mg/kg |
| Administration: | Intravenous injection; daily; for 28 days |
| Result: | Induced a statistically significant increase in overall survival (OS) in mice. |
target
| Target | Value |
| G9a (Cell-free assay) | 8 nM |
| DNMT3A (Cell-free assay) | 85 nM |
| 382 nM | |
| DNMT3B (Cell-free assay) | 1200 nM |
IC 50
G9a: 8 nM (IC50); EHMT1/GLP/KMT1D: 2 nM (IC50); DNMT1: 382 nM (IC50); DNMT3A: 85 nM (IC50); DNMT3B: 1200 nM (IC50)
References
[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. DOI:10.1038/ncomms15424
CM-272 Preparation Products And Raw materials
Raw materials
Preparation Products
CM-272 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Bide Pharmatech Ltd. | 400-164-7117 18317119277 | product02@bidepharm.com | China | 40000 | 60 |
| Shanghai Macklin Biochemical Co.,Ltd. | 15221275939 15221275939 | shenlinxing@macklin.cn | China | 15775 | 55 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4858 | 55 | |
| Shanghai Beckham Medical Technology Co., Ltd | 13816613772 | huahero21@sina.com | China | 2994 | 55 |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9799 | 58 |
| Shanghai YuanYe Biotechnology Co., Ltd. | 15026964105 | 2881489226@qq.com | China | 89667 | 60 |
| ShangHai Biochempartner Co.,Ltd | 177-54423994 17754423994 | 2853530910@QQ.com | China | 8000 | 62 |
| Shanghai SuperLan Chemcial Technique Centre | 0-2022843681 15618226720 | chaolaichem@foxmail.com | China | 9996 | 58 |
| Twochem Co.Ltd. | 021-58111628 15800915896 | sales@twochem.com | China | 1782 | 58 |
| Shanghai Tube Pharmaceutical Co., Ltd. | 021-54338626 18017892860 | sales@tubepharm.com | China | 2709 | 58 |
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