CM-272

Product NameCM-272
CAS1846570-31-7
MFC28H38N4O3
MW478.63
EINECS
MOL File1846570-31-7.mol

Chemical Properties

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

Usage And Synthesis

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

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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

< td style="border-bottom: 1px dotted #ccc;padding: 5px;"> DNMT1
(Cell-free assay)

Target	Value
G9a (Cell-free assay)	8 nM
DNMT3A (Cell-free assay)	85 nM
382 nM
DNMT3B (Cell-free assay)	1200 nM

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