LY-402913 是一种选择性多药耐药蛋白 (MRP1) 抑制剂。

LY-402913 is a selective multidrug resistance protein (MRP1) inhibitor.

LY-402913 inhibits MRP1 and reverses drug resistance to MRP1 substrates, such as doxorubicin, in HeLa-T5 cells (EC50=0.90 μM), while showing no inherent cytotoxicity. LY-402913 inhibits ATP-dependent, MRP1-mediated LTC4 uptake into membrane vesicles prepared from the MRP1-overexpressing HeLa-T5 cells (EC50=1.8 μM). LY-402913 also shows selectivity (~22-fold) against the related transporter, P-glycoprotein, in HL60/Adr and HL60/Vinc cells[2].

When dosed in combination with the oncolytic MRP1 substrate vincristine, LY-402913 delays the growth of MRP1-overexpressing tumors in vivo[2].

334970-65-9

C28H24ClN3O6

533.96

LY 402913;LY402913

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years