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受注：045-509-1970 |
技術サポート：tech@selleck.co.jp 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
化学情報
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Synonyms | XR9576 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C38H38N4O6 |
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| 分子量 | 646.73 | CAS No. | 206873-63-4 | |
| Solubility (25°C)* | 体外 | DMSO | 15 mg/mL (23.19 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | Tariquidar は、CHrB30 細胞株において Kd が 5.1 nM である、P-glycoprotein の強力かつ選択的な非競合阻害剤であり、MDR 細胞株における薬剤耐性を逆転させます。第3相。 |
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| in vitro | Tariquidar displays high-affinity binding to P-gp with Bmax of 275 pmol/mg. This compound shows non-competitive interaction with the P-gp substrates. It 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. This chemical is able to inhibit the vanadate-sensitive ATPase activity of P-gp by 60-70%, with potent IC50 values of 43 nM. It may inhibit other resistance mechanisms at higher concentrations. 1 μM of this compound abrogates ABCG2 (BCRP)-mediated resistance to camptothecins in vitro. It potentiates the cyto-toxicity of several drugs including doxorubicin; complete reversal of resistance is achieved in the presence of 25- 80 nM of this chemical. In MC26, a murine colon carcinoma cell line with intrinsic chemoresistance, the doxorubicin IC50 is fivefold lower in the presence of 0.1 μM of this compound (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 of this chemical. P-gp inhibition persists for 23 h after removal of it from the culture system. It restored the cyto-toxicity of doxorubicin 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 this compound (6 -12 mg/kg p.o.) fully restored the antitumor activity against two highly resistant MDR human tumor xenografts (2780AD, H69/LX4) in nude mice. |
プロトコル(参考用のみ)
| キナーゼアッセイ | Steady-state drug accumulation assay | |
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| Cells are incubated in a reaction volume of 1 mL for 60 min at 37 ℃ under 5% CO2 in order to reach steady-state. The effect of the modulators XR9576 on [3H]-ligand accumulation is investigated in the concentration range 10-9 - 10-6 M. This compound is added from a DMSO stock giving a final solvent concentration of 0.2 % (v/v). Following cell harvesting, accumulated drug is measured by liquid scintillation counting and normalized for cell protein content. Plots of amount accumulated as a function of modulator concentration are fitted with the general dose-response equation: Y={(a-b)/(1+(X/c)d)}+bWhere: Y=response; a=initial response; b=final response; c=EC50 concentration; d=slope value; X=drug concentration. | ||
| 細胞アッセイ | 細胞株 | Murine mammary carcinoma cell line MDR EMT6/AR1.0 |
| 濃度 | ~100 nM Tariquidar | |
| 反応時間 | 4 days | |
| 実験の流れ | Cells are seeded into 96-well plates at 800/well, in 100 μL of medium and incubated for 4 h at 37 ℃. Varying concentrations of this compound or solvent control (50 μL/well) are subsequently added and incubated for an additional 1 h before the addition of the cytotoxic drug. The cytotoxic drug (50 μL) is added to give a range of final concentrations in quadruplicate wells. After incubation for an additional 4 days, cell proliferation of adherent cells is assessed using the sulforhodamine B assay. |
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| 動物実験 | 動物モデル | Murine colon carcinoma xenografts MC26 |
| 投薬量 | 8 mg/kg | |
| 投与方法 | Coadministration of Tariquidar (p.o.) with doxorubicin (5 mg/kg, i.v.) | |
参考
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カスタマーフィードバック
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, , Vet Parasitol, 2015, 211(1-2):80-8.
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Data from [Data independently produced by , , Biochem Pharmacol, 2016, 101:40-53.]
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Data from [Data independently produced by , , Oncotarget, 2017, 8(5):7678-7690]
Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| Second-Generation AURKA-Targeting PROTACs: Structural Optimization toward in Vivo Degradation in Neuroblastoma [ Journal of Medicinal Chemistry, November 18 2025, 23962-23976] | PubMed: 41252673 |
| Low-dose Pimecrolimus, an FDA-approved Calcineurin Inhibitor, Sensitizes Drug-resistant Cancer Cells via Strong P-gp Inhibition [ Anticancer Research, March 15 2023, 1103-1112] | PubMed: 36854528 |
| Overcoming Resistance to Anti–Nectin-4 Antibody-Drug Conjugate [ Molecular Cancer Therapeutics, July 05 2022, 1227-1235] | PubMed: 35534238 |
| Inhibition of P-Glycoprotein Does Not Increase the Efficacy of Proteasome Inhibitors in Multiple Myeloma Cells [ ACS Pharmacology & Translational Science, February 04 2021, 713-729] | PubMed: 33860196 |
| Identification of the Notch ligand DLK1 as an immunotherapeutic target and regulator of tumor cell plasticity and chemoresistance in adrenocortical carcinoma [ Nat Commun, 2025, 16(1):5511] | PubMed: 40595495 |
| Mitochondrial dysfunction fuels drug resistance in adult T-cell acute lymphoblastic leukemia [ J Transl Med, 2025, 23(1):542] | PubMed: 40369632 |
| Fibroblasts Attenuate Anti-Tumor Drug Efficacy in Tumor Cells via Paracrine Interactions with Tumor Cells in 3D Plexiform Neurofibroma Cultures [ Cells, 2025, 14(16)1276] | PubMed: 40862755 |
| Low-Dose Perifosine, a Phase II Phospholipid Akt Inhibitor, Selectively Sensitizes Drug-Resistant ABCB1-Overexpressing Cancer Cells [ Biomol Ther (Seoul), 2025, 33(1):170-181] | PubMed: 39632683 |
| Tumor-acquired somatic mutation affects conformation to abolish ABCG2-mediated drug resistance [ Drug Resist Updat, 2024, 73:101066] | PubMed: 38387283 |
| Enhanced anticancer effect of thymidylate synthase dimer disrupters by promoting intracellular accumulation [ Front Pharmacol, 2024, 15:1477318] | PubMed: 39611169 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。