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CM272
Catalog No.S8812
For research use only.
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. CM-272 prolongs survival in in vivo models of haematological malignancies by at least in part inducing immunogenic cell death.
CAS No. 1846570-31-7
Selleck's CM272 has been cited by 1 Publication
Purity & Quality Control
Choose Selective DNA Methyltransferase Inhibitors
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Biological Activity
| Description | 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. CM-272 prolongs survival in in vivo models of haematological malignancies by at least in part inducing immunogenic cell death. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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. CM-272 inhibits cell proliferation, blocks cell cycle progression and induces apoptosis in ALL, AML and DLBCL cell lines in a dose-dependent manner. CM-272 induces IFN response and immunogenic cell death.[1]. |
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| Cell Data |
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| 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. CM272 shows dose-dependent efficacy and a dose of 2.5 mg/kg of CM272 is adequate to demonstrate the positive anti-tumour efficacy in mice engrafted with ALL-derived CEMO-1 cells.[1]. |
Protocol (from reference)
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Solubility (25°C)
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Chemical Information
| Molecular Weight | 478.63 | ||
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| Formula | C28H38N4O3
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| CAS No. | 1846570-31-7 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | CC1=CC=C(O1)C2=NC3=CC(=C(C=C3C(=C2)NC4CCN(CC4)C)OC)OCCCN5CCCC5 | ||
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Products are for research use only. Not for human use. We do not sell to patients.
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