Name: VEGFR-2/P-gp-IN-1
Brand: TargetMol
SKU: T211172
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

10 mg

待询

50 mg

待询

产品介绍

生物活性

产品描述	VEGFR-2/P-gp-IN-1 is a derivative of Licochalcone A, functioning as an orally active inhibitor of VEGFR-2 (IC50= 0.885 μM) and P-glycoprotein (P-gp). It combats tumor proliferation and overcomes chemotherapy resistance by simultaneously inhibiting VEGFR-2 kinase activity and the P-gp drug efflux pump. This compound suppresses the phosphorylation of VEGFR-2 and proteins in the downstream PI3K/AKT signaling pathway, induces apoptosis, arrests cells in the S phase, and inhibits invasive migration. Additionally, VEGFR-2/P-gp-IN-1 demonstrates potent in vivo antitumor activity in HeLa/DDP cell xenograft models and is applicable in cervical cancer research.
体外活性	VEGFR-2/P-gp-IN-1 (Compound A20) 在不同浓度范围 (1-100 μM, 48 h) 下显著抑制宫颈癌细胞（包括耐药株）的增殖。该化合物 (1-6 μM, 24 h) 通过同时抑制 VEGFR-2 的磷酸化和 P-gp 的外排功能，克服宫颈癌的耐药性。此外，VEGFR-2/P-gp-IN-1 (1-4 μM, 24 h) 可在 HeLa/DDP 细胞中激活细胞凋亡途径，阻断细胞周期在 S 期的进程，从而抑制细胞增殖，并且有效抑制癌细胞的侵袭和迁移。
体内活性	VEGFR-2/P-gp-IN-1 (Compound A20)（10 mg/kg, 20 mg/kg, 40 mg/kg，i.g.，每日一次，持续14天）在HeLa/DDP细胞异种移植小鼠模型中展现了治疗顺铂耐药性宫颈癌的潜力，并且具有良好的安全性，没有显著毒性。