| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| T408367-1ml |
1ml |
现货  |
|
| 英文别名 | 3-Quinolinecarboxamide, N-[2-[[[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]amino]carbonyl]-4,5-dimethoxyphenyl]- |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Tariquidar (XR9576) |
| 生化机理 | Tariquidar (XR9576) 是一种强效、选择性的 P 糖蛋白非竞争性抑制剂，在 CHrB30 细胞系中的Kd为 5.1 nM，可逆转 MDR 细胞系的耐药性。3 期 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | P 糖蛋白 1 抑制剂 |
| 产品介绍 |
Information Tariquidar (XR9576) Tariquidar (XR9576) is a potent and selective noncompetitive inhibitor of P-glycoprotein with K d of 5.1 nM in CHrB30 cell line, reverses drug resistance in MDR cell Lines. Phase 3. 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 CHrB30 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). In murine mammary carcinoma, human small-cell lung carcinoma and human ovarian carcinoma cell lines with acquired chemotherapeutic resistance (EMT6/AR1.0, H69/LX4 and 2780 AD), the in vitro doxorubicin IC50 is 22-150-fold lower in the presence of 0.1 μM Tariquidar. P-gp inhibition persists for 23 h after removal of Tariquidar from the culture system. Tariquidar restored the cyto-toxicity of doxorubicin and vinblastine in the National Cancer Institute (NCI)/ADRRES multicellular tumor spheroid model derived from the MCF7WT breast cancer cell line. In vivo Tariquidar (2- 8 mg/kg p.o.) is found to significantly potentiate the antitumor activity of doxorubicin (5 mg/kg, i.v.) against MC26 murine colon carcinoma in vivo. In human carcinoma xenografts, coadministration of XR9576 (6 -12 mg/kg p.o.) fully restored the antitumor activity of paclitaxel, etoposide, and vincristine against two highly resistant MDR human tumor xenografts (2780AD, H69/LX4) in nude mice. cell lines： Concentrations：~100 nM Tariquidar Incubation Time：4 days Powder Purity:≥99% |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | COC1=CC2=C(CN(CCC3=CC=C(NC(=O)C4=C(NC(=O)C5=CC6=CC=CC=C6N=C5)C=C(OC)C(=C4)OC)C=C3)CC2)C=C1OC |
| 分子量 | 646.73 |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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