Bioactivity | CYP4Z1-IN-1 (compound 7c) is a potent CYP4Z1 inhibitor, with an IC50 of 41.8 nM. CYP4Z1-IN-1 decreases the expression of breast CSCs stemness markers, spheroid formation, and metastatic ability as well as tumor-initiation capability in a concentration-dependent manner in vitro and in vivo[1]. |
Invitro | CYP4Z1-IN-1 (compound 7c) 显示出对乳腺 CSC (癌症干细胞)的抗增殖活性,IC50 为 483 ± 2.5 nM[1] 。CYP4Z1-IN-1 (0.8-51.2 μM, 24 h) 抑制乳腺癌细胞中干细胞标记物 (P-gp, Oct3/4, Nanog, ALDH1A1, 和 Sox2) 的表达[1]。CYP4Z1-IN-1 (0.8-51.2 μM, 24-48 h) 可减弱乳腺癌细胞的迁移和侵袭能力[1]。 Western Blot Analysis[1] Cell Line: |
In Vivo | CYP4Z1-IN-1 (compound 7c) (2000 mg/kg,口服,连续 7 天)对小鼠没有明显的毒性和体重减轻[1]。CYP4Z1-IN-1 (12.8 μM, 72 h处理MCF-7 and MDA-MB-231 cells,然后细胞皮下植入小鼠腹股沟乳腺) 可阻断乳腺癌细胞的肿瘤启动能力[1]。 Animal Model: |
Name | CYP4Z1-IN-1 |
CAS | 2760611-38-7 |
Formula | C13H18N2O3 |
Molar Mass | 250.29 |
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]. Yuan Y, et al. Identification of a Novel Potent CYP4Z1 Inhibitor Attenuating the Stemness of Breast Cancer Cells through Lead Optimization. J Med Chem. 2022 Dec 8;65(23):15749-15769. |