CM272

CM272 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.TargetsG9a (Cell-free assay); DNMT3A (Cell-free assay); DNMT1 (Cell-free assay); DNMT3B (Cell-free assay) 8 nM ;85 nM; 382 nM; 1200 nMIn vitroThe GI50 for CM-272 after 48\u2009h 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..In vivoCM272 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\u2009week of treatment and no significant weight loss is observed in treated animals. CM272 shows dose-dependent efficacy and a dose of 2.5\u2009mg/kg of CM272 is adequate to demonstrate the positive anti-tumour efficacy in mice engrafted with ALL-derived CEMO-1 cells..Cell Research(from reference)Cell lines：ALL, AML, DLBCL, CEMO-1, LAL-CUN-2, MV4-11, OCI-AML-2, OCI-Ly3, OCI-Ly10 cell lines Incubation Time：24, 48, 72 and 96h

DNA Methyltransferase Inhibitors

Specifications & Purity: CM272 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.TargetsG9a (Cell-free assay); DNMT3A (Cell-free assay); DNMT1 (Cell-free assay); DNMT3B (Cell-free assay) 8 nM ;85 nM; 382 nM; 1200 nMIn vitroThe GI50 for CM-272 after 48\u2009h 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..In vivoCM272 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\u2009week of treatment and no significant weight loss is observed in treated animals. CM272 shows dose-dependent efficacy and a dose of 2.5\u2009mg/kg of CM272 is adequate to demonstrate the positive anti-tumour efficacy in mice engrafted with ALL-derived CEMO-1 cells..Cell Research(from reference)Cell lines：ALL, AML, DLBCL, CEMO-1, LAL-CUN-2, MV4-11, OCI-AML-2, OCI-Ly3, OCI-Ly10 cell lines Incubation Time：24, 48, 72 and 96h

Molecular Formula: C28H38N4O3 

Molecular Weight: 478.63

PubChem CID: 118607432

Isomeric SMILES: CC1=CC=C(O1)C2=NC3=CC(=C(C=C3C(=C2)NC4CCN(CC4)C)OC)OCCCN5CCCC5

Storage Temperature: Store at -20°C

Shipped in: Ice chest + Ice pads

More Information: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/C414197-SCI_2bf26010266dbc42cf2bc1299257761b.pdf

UPC:

51442705

Weight:

1.06 Ounces

HazmatClass:

Yes

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

C414197-1mg

Country of Origin:

China

CAS:

1846570-31-7

Product Size:

1mg

Harmonized Tariff Code:

2931.90.90

Hazard Statement Codes:

H302;H315;H319;H335

Precautionary Statement Codes:

P261;P280;P301+P312;P302+P352;P305+P351+P338