Bioactivity | 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]. |
Invitro | 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: |
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: |
Name | Antitumor agent-88 |
CAS | 1422527-87-4 |
Formula | C23H30N2O7S |
Molar Mass | 478.56 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |