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  • DC Chemicals Limited
  • China
  • Product Name: CHM-1
  • Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

154554-41-3

154554-41-3 structure
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
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

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154554-41-3 structure

154554-41-3

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

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154554-41-3 structure

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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154554-41-3 structure

154554-41-3

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