The differences were dethermione with Student’s t-test. Significance was set at p 0.05. Third Results 3.1. Reverse MDR by FG020326 ALK Pathway in vitro As shown in Table 1, MCF-7 cells adr 176, 68 and 49 times the resistance at Dox, VCR and paclitaxel exposed compared to parental MCF-7 cells. KBv200 cells were 49, 47 and 35-fold resistance to Dox, VCR and paclitaxel, compared with parental KB cells. Comparison of cells were S1 S1 M1 80 143.2 cells resistant to topotecan. KB-CV60 cells were 12 times more resistant to VCR by parents KB 3 1 cells. 2R120 SW1573 cells were 13 times more resistant to doxorubicin compared to his parents SW1573 cells and NIH3T3 cells MRP4 2 were 22-times more resistant.
Against VCR compared to its parent NIH 3T3 cells Mediated Before examining zafirlukast the effectiveness of FG020326 to ABCB1, ABCC1, ABCC4, ABCG2, and LRP Undo MDR in cancer cells Ngig to make, we have the first cytotoxicity t evaluated by FG020326 in various cell lines using the MTT assay. IC50 values were tested by FG020326 for cell lines 50 overall cell survival was 90 sts used in all cell lines at the concentrations in this experiment for MDR reversal. FG020326 1.25, 2.5 and 5.0 M produces a concentration–Dependent increase in cytotoxicity t of doxorubicin, VCR and paclitaxel in MDR cells overexpress ABCB1, including normal MCF-7 cells and KBv200 adr. However FG020326 had no significant effect on the improvement of the cytotoxicity t In drug-sensitive parental cells, including normal MCF-7, KB, KB 1 3, NIH3T3, S1 and SW1573 cells or Reverse Rtsfahren MDR caused by ABCC1, ABCC4 , ABCG2, and LRP.
Moreover, not much Change FG020326 IC50 values of 5 fluoropyrimidine and cisplatin, not the ABCB1 substrates in MDR cells ABCB1 expression. 3.2. Reverse MDR by FG020326 in KBv200 cell xenograft KBv200 xenograft cells was used to determine the F Determine ability to reverse FG020326 MDR in vivo. As shown in Figure 1, the results show that neither FG020326 paclitaxel VCR alone a significant effect on the growth of xenograft KBv200 cells had. However, the combination of paclitaxel FG020326 and VCR or a significant inhibition of the growth of xenografts and the inhibition was 46.7 and 51.7, respectively. In addition, mortality was no t or a decrease in the K Rpergewichts associated with combination therapy, suggesting that the combination therapy is not obtained Hter toxicity Lead t. 3.3.
Plasma FG020326 at M Usen to best Term whether FG020326 k Nnte plasma levels required to achieve MDR in vivo Undo Ngig, we measure plasma concentrations NIH M Usen after its po administration. The BC administration of 100 mg kg FG020236 produced a maximum plasma concentration of 5.3 M. Au Addition, a plasma concentration of 1.24 M FG020236 reached 8 hours after administration. Moreover, the concentration of yet sufficient to reverse drug resistance by 12 clock FG020326