P-gp inhibitor 5 (compound 10) 是一种有效的P 糖蛋白 (P-gp)抑制剂,在 1.25 μM 和 2.5 μM 时 P-gp 抑制倍数分别为 2.5 和 3.0。P-gp inhibitor 5 对某些癌细胞有抗增殖活性。P-gp inhibitor 5 可通过恢复细胞对 Vincristine 和 Paclitaxel 的敏感性,有效逆转 ABCB1/Flp-InTM-293 和 KBvin 的多药耐药 (MDR) 表型。
产品描述
P-gp inhibitor 5 (compound 10) is a potent P-glycoprotein (P-gp) inhibitor with P-gp inhibition fold of 2.5 and 3.0 at 1.25 μM and 2.5 μM. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-In TM -293 and KBvin cells by restoring their sensitivity to Vincristine and Paclitaxel [1].
体外活性
P-gp inhibitor 5 (compound 10) has cytotoxic against ABCB1/Flp-In TM -293 and KBvin cells with IC 50 s of 29.7 and 12.6 μM, respectively [1]. P-gp inhibitor 5 (2.5 and 5 μM) lows the IC 50 s of KBvin cells for Vincristine to 7.59~36.82 nM, for Paclitaxel to 21.0~79.5 nM, for Doxorubicin to 85.7~111 nM; lows the IC 50 s of HeLaS3 cells for Vincristine to 2.24~3.91 nM, for Paclitaxel to 8.81~9.58 nM, for Doxorubicin to 102~1260 nM [1].
Cas No.
2451298-06-7
分子式
C28H20ClNO5S
分子量
517.98
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years