Tariquidar

製品コードS8028 バッチS802803

印刷

化学情報

Chemical Structure Synonyms XR9576 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C38H38N4O6
分子量 646.73 CAS No. 206873-63-4
Solubility (25°C)* 体外 DMSO 5.6 mg/mL (8.65 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.280mg/ml (0.43mM) Taking the 1 mL working solution as an example, add 50 μL of 5.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Tariquidar is a potent and selective noncompetitive inhibitor of P-glycoprotein with Kd of 5.1 nM in CHrB30 cell line, reverses drug resistance in MDR cell Lines. Phase 3.
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. [1] It may inhibit other resistance mechanisms at higher concentrations. 1 μM of this compound abrogates ABCG2 (BCRP)-mediated resistance to camptothecins in vitro. [2] 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. [3] 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. [4]
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. [3]

プロトコル(参考用のみ)

キナーゼアッセイ Steady-state drug accumulation assay
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.
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

  • https://pubmed.ncbi.nlm.nih.gov/10510451/
  • https://pubmed.ncbi.nlm.nih.gov/14973080/
  • https://pubmed.ncbi.nlm.nih.gov/11212278/
  • https://pubmed.ncbi.nlm.nih.gov/14962729/

カスタマーフィードバック

, , Vet Parasitol, 2015, 211(1-2):80-8.

Data from [Data independently produced by , , Biochem Pharmacol, 2016, 101:40-53.]

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：

Mitochondrial dysfunction fuels drug resistance in adult T-cell acute lymphoblastic leukemia [ J Transl Med, 2025, 23(1):542] PubMed: 40369632
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
Zosuquidar: An Effective Molecule for Intracellular Ca2+ Measurement in P-gp Positive Cells [ Int J Mol Sci, 2024, 25(6)3107] PubMed: 38542082
Cellular uptake of CPX-351 by scavenger receptor class B type 1-mediated nonendocytic pathway [ Exp Hematol, 2024, S0301-472X(24)00516-2] PubMed: 39362576
Ivermectin Enhances Paclitaxel Efficacy by Overcoming Resistance Through Modulation of ABCB1 in Non-small Cell Lung Cancer [ Anticancer Res, 2024, 44(12):5271-5282] PubMed: 39626921
The net electrostatic potential and hydration of ABCG2 affect substrate transport [ Nat Commun, 2023, 14(1):5035] PubMed: 37596258
The net electrostatic potential and hydration of ABCG2 affect substrate transport [ Nat Commun, 2023, 14(1):5035] PubMed: 37596258
MDR1 Inhibition Reverses Doxorubicin-Resistance in Six Doxorubicin-Resistant Canine Prostate and Bladder Cancer Cell Lines [ Int J Mol Sci, 2023, 24(9)8136] PubMed: 37175843

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。

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