CM-272

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CM-272 (CM272) 是一种新型有效、选择性和可逆的 G9a/DNMT 双重抑制剂，对 G9a 和 DNMT1 的 IC50 分别为 8 nM 和 382 nM。

CM-272 (CM272)?is a novel potent, selective and reversible dual inhibitor of G9a/DNMTs with IC50 of 8 nM and 382 nM for G9a and DNMT1, respectively; also inhibits DNMT3A/3B/GLP with IC50 of 85/1,200/2 nM, respectively; inhibits cell proliferation and promotes apoptosis in different haematological neoplasias (AML, ALL and DLBCL); significantly prolongs survival of AML, ALL and DLBCL xenogeneic models.

Cell Proliferation AssayCell Line:CEMO-1, MV4-11 and OCI-Ly10 cell linesConcentration: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: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-dependent manner.

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.

CM272 | CM 272

Chromatin/Epigenetic

HMTase

HMTase

Cancer

——

1846570-31-7

478.637

C28H38N4O3

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (261.16 mM)

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

6-methoxy-2-(5-methylfuran-2-yl)-N-(1-methylpiperidin-4-yl)-7-(3-(pyrrolidin-1-yl)propoxy)quinolin-4-amine

(-20℃)

With Ice Pack

≥ 2 years