CM-272

SKU: orb1225855

Description

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.

Key Properties

• CAS Number: 1846570-31-7
• MW: 478.637
• Purity: >98% (HPLC)
• Formula: C₂₈H₃₈N₄O₃
• SMILES: CC1=CC=C(O1)C2=NC3=CC(=C(C=C3C(=C2)NC4CCN(CC4)C)OC)OCCCN5CCCC5
• Target: HMTase
• Solubility: In Vitro: DMSO : 125 mg/mL (261.16 mM)

Bioactivity

• In Vivo:
  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.
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• In Vitro:
  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: 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CM272 | CM 272

Quick Database Links

Gene Symbol

HMTase