Antitumor agent-87

Antitumor agent-87 is a potent antitumor agent. Antitumor agent-87 shows a high affinity for CYP1A1 with a Ki value of 0.23 µM. Antitumor agent-87 shows antiproliferative activity. Antitumor agent-87 induces cell cycle arrest at the G2/M phase. Antitumor agent-87 show antitumoral activity[1].

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450

CYP1A1:0.23 μM (Ki)

Antitumor agent-87 (compound 10) 在人肝微粒体、小鼠肝微粒体和大鼠肝微粒体中的半衰期 (t1/2) 分别为 70、44、107 分钟[1]。 Antitumor agent-87 (1250 nM) 诱导细胞周期停滞在 G2/M 期[1]。 Antitumor agent-87 (0-12500 nM; 72 h) 具有抗增殖活性，对 HT-1080CYP1A1, HT-1080empty, HT-1080, MDA-MB-231, MDA-MB-468, T47D, SK-BR-3, MCF7细胞的 IC50 值分别为 500, 8800, 6800, >12500, 210, 1100, 79, 43 nM[1]。 Cell Proliferation Assay[1] Cell Line: MCF7, HT-29, M21 cells Concentration: 0-12500 nM Incubation Time: 48 h Result: Showed antiproliferative activity with IC50s of 600, >12500, >12500 nM for MCF7, HT-29, M21 cells, respectively. Cell Cycle Analysis[1] Cell Line: MCF7 cells Concentration: 1250 nM Incubation Time: Result: Induced the accumulation of the cells in the G2/M phase of 57% and induced disruptions of the cytoskeleton of MCF7 cells.

Antitumor agent-87 (0.1 µg/egg) 在鸡胚中表现出抗肿瘤活性[1]。 Animal Model: chick embryos (HT-1080CYP1A1, HT-1080empty, HT-1080 cells)[1] Dosage: 0.1 µg/egg Administration: Result: Did not show statistically significant antitumor activity on grafted cell lines devoid of CYP1A1 (HT-1080 and HT-1080empty), showed antitumoral inhibition of 29% on the grafted HT-1080CYP1A1.

[1]. Chavez Alvarez AC, et al. Homologation of the Alkyl Side Chain of Antimitotic Phenyl 4-(2-Oxo-3-alkylimidazolidin-1-yl)benzenesulfonate Prodrugs Selectively Targeting CYP1A1-Expressing Breast Cancers Improves Their Stability in Rodent Liver Microsomes. J Med Chem. 2023 Feb 23;66(4):2477-2497.