Antitumor agent-88

Names

[ Name ]:
Antitumor agent-88

Biological Activity

[Description]:

Antitumor agent-88 exhibits potent antimitotic activity and arrests cell in the G2/M phase. Antitumor agent-88 disrupts the microtubule and the cytoskeleton in CYP1A1-expressing breast cancer cells. Antitumor agent-88 is also a competitive inhibitor of CYP1A1 (Ki: 1.4 μM)[1].

[Related Catalog]:

Research Areas >> Cancer

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

[Target]

CYP1A1:1.4 μM (Ki)

[In Vitro]

Antitumor agent-88 (Compound 14, 48 h) 抑制 MCF-7 细胞生长，IC50 为 200 nM，对 MDA-MB-231 (IC50 >8600 nM)[1]。 Antitumor agent-88 抑制 MDA-MB-468、SK-BR 细胞生长，IC50 分别为 21 nM、3.2 nM[1]。 Antitumor agent-88 (50 nM, 48 h) 导致 42% 细胞在 G2/M 期停滞[1]。 Antitumor agent-88 对 CYP1A1 具有高亲和力 (Ki: 1.4 μM)[1]。 Antitumor agent-88 选择性抑制 HT-1080 细胞增殖，对转染 CYP1A1 的 HT-1080 的 IC50 为 30 nM[1]。 Cell Viability Assay[1] Cell Line: MCF-7 cell Concentration: 50 nM Incubation Time: 48 h Result: Arrested cell in G2/M phase.

[In Vivo]

Antitumor agent-88 (化合物 14) (1 μg/蛋) 在携带 HT-1080CYP1A1 肿瘤的鸡胚中显示出抗肿瘤活性[1]。 Animal Model: Chick embryos grafted with HT-1080CYP1A1 cells[1] Dosage: 1 μg/egg Administration: Applied to chick chorioallantoic membrane. Result: Reduced tumor weight by 49%.

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₃H₃₀N₂O₇S

[ Molecular Weight ]:
478.56

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.