Tariquidar
| CAS号 | 206873-63-4 | 货号 | BCP06102 |
| 中文名 | Tariquidar | ||
| 英文名 | Tariquidar | ||
| 中文别名 | |||
| 英文别名 | XR 9576;XR-9576;XR9576; | ||
| 分子式 | C38H38N4O6 | 分子量 | 646.73 |
| 生物活性 | Tariquidar displays high-affinity binding to P-gp with Bmax of 275 pmol/mg. Tariquidar shows non-competitive interaction with the P-gp substrates vinblastine and paclitaxel. Tariquidar increases the steady-state accumulation of these cytotoxics in CHr<>/supB30 cells to levels observed in non-P-gp-expressing AuxB1 cells with EC50 of 487 nM. Tariquidar is able to inhibit the vanadate-sensitive ATPase activity of P-gp by 60-70%, with potent IC50 values of 43 nM. Tariquidar may inhibit other resistance mechanisms at higher concentrations. 1 μM Tariquidar abrogates ABCG2 (BCRP)-mediated resistance to camptothecins in vitro. Tariquidar potentiates the cyto-toxicity of several drugs including doxorubicin, paclitaxel, etoposide, and vincristine; complete reversal of resistance is achieved in the presence of 25- 80 nM Tariquidar. In MC26, a murine colon carcinoma cell line with intrinsic chemoresistance, the doxorubicin IC50 is fivefold lower in the presence of 0.1 μM Tariquidar (36 vs 7 nM). | ||
| 信号通路 | Ion Channel/Membrane Transporter Neuro Signaling Pathway | ||
| 靶 点 | P glycoprotein | ||
结构式
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