Bioactivity | PS121912 is a selective vitamin D receptor (VDR)-coregulator inhibitor. PS121912 has acceptable metabolic stability in vivo. PS121912 can be used for the research of cancer[1]. |
Invitro | PS121912 在低浓度下表现得像 VDR 拮抗剂,但在高浓度下与更多靶标相互作用,导致半胱天冬酶 3/7 激活介导的细胞凋亡[1]。PS121912(与 1,25-(OH)2D3 结合)降低细胞周期蛋白 A 和 D 的转录水平,从而使 HL-60 细胞停滞在 S 期或 G2/M 期[1]。 Cell Viability Assay[1] Cell Line: |
In Vivo | PS121912 表现出可接受的代谢稳定性,在体内癌症研究中可以在较高浓度下抑制代谢酶 CYP3A4[1]。 |
Name | PS121912 |
CAS | 1529814-60-5 |
Formula | C24H21F3N2O |
Molar Mass | 410.43 |
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]. Sidhu PS, et al. Anticancer activity of VDR-coregulator inhibitor PS121912. Cancer Chemother Pharmacol. 2014;74(4):787-798. |