CHM1

Names

[ Name ]:
CHM1

[Synonym ]:
2-(2-fluorphenyl)-6,7-methylenedioxyquinolin-4-one
1,3-Dioxolo[4,5-g]quinolin-8(5H)-one,6-(2-fluorophenyl)
2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one
2'-fluoro-6,7-methylenedioxy-2-phenyl-4-quinolone
6-(2-fluorophenyl)-[1,3]-dioxolo[4,5-g]quinolin-8(5H)-one
CHM-1
2-(2-fluorophenyl)-6,7-methylenedioxy-2-4-quinolone hydrate

Biological Activity

[Description]:

CHM-1, a microtubule-destabilizing agent, inhibits tubulin polymerization. CHM-1 is a potent and selective antimitotic antitumor activity against human hepatocellular carcinoma. CHM-1 induces growth inhibition and apoptosis via G2-M phase arrest in human hepatocellular carcinoma cells by activation of Cdc2 kinase activity[1][2][3].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin

Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin

[Target]

IC50: 0.75 μM (HA22T)[1]

[In Vitro]

CHM-1 (0-100μM; 24 hours) induces significant concentration-dependent growth inhibition in HA22T, Hep3B, and HepG2 cells, with the most potent effects observed in HA22T cells (IC50 = 0.75 μM)[1]. CHM-1 (0-10 μM; 24 hours) significantly increases the binding of cyclin B1 to Cdc2 in HA22T cells[1]. Cell Viability Assay[1] Cell Line: HA22T, Hep3B, and HepG2 cells Concentration: 0-100 μM Incubation Time: 24 hours Result: Induced G2-M arrest of the cell cycle followed by apoptosis. Western Blot Analysis[1] Cell Line: HA22T cells Concentration: 0-10 μM Incubation Time: 24 hours Result: Induced change in expressed and phosphorylated status of G2-M regulators in human hepatocellular carcinoma cells.

[In Vivo]

CHM-1 (10 mg/kg; I.p.) induces a dose-dependent inhibition of HA22T tumor growth[1]. Animal Model: Male severe combined immunodeficient mice (HA22T)[1] Dosage: 10 mg/kg Administration: I.p. Result: Induced a dose-dependent inhibition of HA22T tumor growth.

[References]

[1]. Wang SW, et al. CHM-1, a novel synthetic quinolone with potent and selective antimitotic antitumor activity against human hepatocellular carcinoma in vitro and in vivo. Mol Cancer Ther. 2008 Feb;7(2):350-60.

[2]. Liu CW, et al. CHM-1, a novel microtubule-destabilizing agent exhibits antitumor activity via inducing the expression of SIRT2 in human breast cancer cells. Chem Biol Interact. 2018 Jun 1;289:98-108.

[3]. Tsai AC, et al. CHM-1, a new vascular targeting agent, induces apoptosis of human umbilical vein endothelial cells via p53-mediated death receptor 5 up-regulation. J Biol Chem. 2010 Feb 19;285(8):5497-506.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₆H₁₀FNO₃

[ Molecular Weight ]:
283.25400

[ Exact Mass ]:
283.06400

[ PSA ]:
51.32000

[ LogP ]:
3.06290

MSDS

Click to get detail MSDS

Synthetic Route

Click to get detail synthetic route

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.