|
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
|
Synonyms | GW120918, GG918, GW0918 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
|||
| 化学式 | C34H33N3O5 |
||||||
| 分子量 | 563.64 | CAS No. | 143664-11-3 | ||||
| Solubility (25°C)* | 体外 | DMSO (warmed with 50ºC water bath) | 100 mg/mL (177.41 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） |
|
||||||
|
* <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 | Elacridar (GF120918, GW120918, GG918, GW0918) is a potent P-gp (MDR-1) and BCRP inhibitor. |
|---|---|
| in vitro | Elacridar (GF120918) inhibits P-glycoprotein (P-gp) labeling by [3H]azidopine with a IC50 of 0.16 μM. [2] In Caki-1 and ACHN cells, it ( 2.5 μM) significantly ihibits the cell growth. The P-glycoprotein activity is found to be inhibited by this compound. Its combination lead to a significant reduction in ABC Sub-family B Member 2 (ABCG2) expression in 786-O cells. [3] |
| in vivo | Elacridar (GF120918) increases plasma and brain concentrations and brain-to-plasma ratios in wild-type mice when co-administered orally (100 mg/kg, p.o.), equaling the levels in Abcb1a/1b; Abcg2-/- mice. [1] In friend leukemia virus stain B mice, the brain-to-plasm partition coefficient (Kp, brain) of this compound is 0.82, 0.43, and 4.31 after intravenous (2.5 mg/kg), intraperitoneal (100 mg/kg), and oral (100 mg/kg) treatment, respectively. [4] In Mrp4(-/-) mice, it fully inhibits P-gp mediated transport, without siginificant effects on Bcrp1-mediated transport. [5] |
プロトコル(参考用のみ)
| キナーゼアッセイ | Photoaffinity radiolabeling of P-gp | |
|---|---|---|
| 10 μL of unlabeled cell membrane suspension (at 0.4 mg of protein/mL) are aliquoted into each well in 96-well plates. 5 μL of Elacridar (GF120918) are then added to each well. The plate is incubated 25 min at 25℃ in the dark. 5 μL of tritiated azidopine (1.8 TBq/mmol) (0.6 μM in HCI 0.2 mM) are added to each well. After 25 min of incubation at 25℃ in the dark, samples are simultaneously irradiated for 2 min at 254 nm at 0℃ with a thin layer chromatography-designed UV lamp directly in contact with the plate. Samples are solubilized in sodium dodecyl sulfate-polyacrylamide gel electrophoresis sample buffer but not heated. After separation on a 7.5% polyacrylamide gel, the gel is treated for fluorography with Amplify and exposed during 3 days onto a photosensitive film. The fluorography is analysed using a Camag thin layer chromatography Scanner II densitometer. | ||
| 細胞アッセイ | 細胞株 | ACHN, Caki-1, 786-O, and MCF-7 cells |
| 濃度 | ~ 5 mM | |
| 反応時間 | 48 h | |
| 実験の流れ | After seeding 3.0×10³ cells per well in a 96-well plate and incubating for 24 h, an optimum concentration gradient of Elacridar (GF120918) is added to each well. Following a 48 h culture period, cell viability is assessed using the proliferation reagent, MTT. Control cells are treated with the vehicle only, 0.1% DMSO. After this final incubation, the medium is aspirated and precipitated formazan crystals are dissolved in DMSO (100 µL/well). The absorbance of each well is measured at 540 nm, and a reference wavelength of 650 nm is read with a multiskan JX microplate reader. Cell viability is calculated as percentage of the control value. |
|
| 動物実験 | 動物モデル | Male wild-type, Abcb1a/1b-/-34, Abcg2 -/-32 and Abcb1a/1b;Abcg2 |
| 投薬量 | 100 mg/kg | |
| 投与方法 | p.o. | |
参考
|
カスタマーフィードバック
-
Data from [Data independently produced by , , J Exp Clin Cancer Res, 2017, 36(1):122]
-
Data from [Data independently produced by , , Biochem Pharmacol, 2016, 101:40-53.]
-
Data from [Data independently produced by , , Biochem Pharmacol, 2016, 101:40-53]
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：
| Screening a living biobank identifies cabazitaxel as a strategy to combat acquired taxol resistance in high-grade serous ovarian cancer [ Cell Rep Med, 2025, 6(6):102160] | PubMed: 40466638 |
| Synthesis of carbon dots from spent coffee grounds: transforming waste into potential biomedical tools [ Nanoscale, 2025, 17(16):9947-9962] | PubMed: 40067158 |
| Nbeal2 Inactivation Triggers Abl1 Stabilisation and Dysregulated Subcellular Localisation of the Multi-Drug-Resistant Protein MDR1 (ABCB1) in Mast Cells [ Immunology, 2025, NONE] | PubMed: 41111259 |
| Targeting SUMOylation in ovarian cancer: Sensitivity, resistance, and the role of MYC [ iScience, 2025, 28(6):112555] | PubMed: 40487451 |
| Elacridar Inhibits BCRP Protein Activity in 2D and 3D Cell Culture Models of Ovarian Cancer and Re-Sensitizes Cells to Cytotoxic Drugs [ Int J Mol Sci, 2025, 26(12)5800] | PubMed: 40565261 |
| The Role of Elacridar, a P-gp Inhibitor, in the Re-Sensitization of PAC-Resistant Ovarian Cancer Cell Lines to Cytotoxic Drugs in 2D and 3D Cell Culture Models [ Int J Mol Sci, 2025, 26(3)1124] | PubMed: 39940891 |
| Overcoming ABCB1 mediated multidrug resistance in castration resistant prostate cancer [ Cell Death Dis, 2024, 15(8):558] | PubMed: 39090086 |
| Targeting the glutamine metabolism to suppress cell proliferation in mesenchymal docetaxel-resistant prostate cancer [ Oncogene, 2024, 43(26):2038-2050] | PubMed: 38750263 |
| Abcg2a is the functional homolog of human ABCG2 expressed at the zebrafish blood-brain barrier [ Fluids Barriers CNS, 2024, 21(1):27] | PubMed: 38491505 |
| 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。