<Suppliers Price>

CHM1

Names

[ CAS No. ]:
154554-41-3

[ 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