Antiproliferative agent-23_product_DataBase

Bioactivity	Antiproliferative agent-23 is a microtubule-destabilizing agent (MDA) and efficiently disturbes the tubulin-microtubule system. Antiproliferative agent-23 induces apoptosis via a mitochondrion-dependent pathway by downregulating the Bcl-2 protein, upregulating Bax and Cyt c proteins, and activating the caspase cascade. Antiproliferative agent-23 initiates reactive oxygen species (ROS)-mediated endoplasmic reticulum stress in A549/CDDP cells (cisplatin resistant cancer cell line) via the PERK/ATF4/CHOP signaling pathway. Antiproliferative agent-23 has anti-tumor activity[1].
Invitro	Antiproliferative agent-23 (72 小时) 对 HepG2 (IC50=0.86)、MDA-MB-231 (IC50=1.53)、MCF-7 (IC50=0.94)、A2780 (IC50=0.88)、A549 (IC50=0.23)、A549/CDDP (IC50=0.35)、HepG2/CDDP (IC50=1.16)、HUEVC (IC50=5.68) 具有抗增殖作用[1]。Antiproliferative agent-23 (5 μM; 24 小时) 有效诱导 A549/CDDP 细胞凋亡[1]。Antiproliferative agent-23 (5 μM; 24小时) 可以有效地引起 A549/CDDP 细胞的 DNA 损伤，从而最终引发细胞凋亡。Antiproliferative agent-23 导致 ER 应激相关蛋白表达显着增加[1]。Antiproliferative agent-23 (10, 20 μM; 24 小时) 导致聚合抑制作用，ic50 为 9.86 μM[1]。Antiproliferative agent-23 (5 μM; 24小时) 显着增加 A549/CDDP 细胞中的细胞内 ROS[1]。Antiproliferative agent-23 (1 μM; 24 小时) 在体外试验中有效抑制 A549 细胞迁移[1]。 Apoptosis Analysis[1] Cell Line:
In Vivo	Antiproliferative agent-23 (12.40 mg/kg; 静脉给药; 每 7 天一次; 连续 28 天) 具有抗肿瘤功效并保持高抗肿瘤效率以减弱 CDDP 抗性[1]。 Animal Model:
Name	Antiproliferative agent-23
Formula	C23H28Cl3N3O6Pt
Molar Mass	743.93
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]. Zhikun Liu, et al. Novel Indole-Chalcone Derivative-Ligated Platinum(IV) Prodrugs Attenuate Cisplatin Resistance in Lung Cancer through ROS/ER Stress and Mitochondrial Dysfunction. J Med Chem. 2023 Apr 13;66(7):4868-4887.

PeptideDB

Antiproliferative agent-23

CAS: F: C23H28Cl3N3O6Pt W: 743.93