CHM-1  (Synonyms: NSC656158)

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].

IC50: 0.75 μM (HA22T)^[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CHM-1 (10 mg/kg; I.p.) induces a dose-dependent inhibition of HA22T tumor growth^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

283.25

C₁₆H₁₀FNO₃

154554-41-3

固体

Off-white to light yellow

Room temperature in continental US; may vary elsewhere.

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• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]