154554-41-3

154554-41-3 structure

Name: CHM1
Chemical Name: 6-(2-fluorophenyl)-5H-[1,3]dioxolo[4,5-g]quinolin-8-one
CAS Number: 154554-41-3
Molecular Formula: C₁₆H₁₀FNO₃
Molecular Weight: 283.25400
Catalog: Signaling Pathways Cell Cycle/DNA Damage Microtubule/Tubulin
Create Date: 2016-12-11 15:24:32
Modify Date: 2024-01-07 09:47:04
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].

Name	6-(2-fluorophenyl)-5H-[1,3]dioxolo[4,5-g]quinolin-8-one
Synonyms	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

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.

Molecular Formula	C₁₆H₁₀FNO₃
Molecular Weight	283.25400
Exact Mass	283.06400
PSA	51.32000
LogP	3.06290

666818-14-0

154554-41-3

Literature: Xia; Yang; Hackl; Hamel; Mauger; Wu; Lee Journal of Medicinal Chemistry, 2001 , vol. 44, # 23 p. 3932 - 3936

28657-75-2

154554-41-3

Literature: Li; Wang; Kuo; Wu; Lednicer; Lin; Hamel; Lee - Journal of Medicinal Chemistry, 1994 , vol. 37, # 8 p. 1126 - 1135

393-52-2

154554-41-3

Literature: Li; Wang; Kuo; Wu; Lednicer; Lin; Hamel; Lee - Journal of Medicinal Chemistry, 1994 , vol. 37, # 8 p. 1126 - 1135

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