Elacridar (GF120918)

製品コードS7772 バッチS777204

印刷

化学情報

Chemical Structure 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 3 mg/mL warmed with 50ºC water bath (5.32 mM)
Water Insoluble
Ethanol Insoluble
* <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 inhibits P-glycoprotein (P-gp) labeling by [3H]azidopine with a IC50 of 0.16 μM. [2] In Caki-1 and ACHN cells, elacridar ( 2.5 μM) significantly ihibits the cell growth. The P-glycoprotein activity is found to be inhibited by elacridar. The combination of elacridar and sunitinib lead to a significant reduction in ABC Sub-family B Member 2 (ABCG2) expression in 786-O cells. [3]
in vivo Oral co-administration of elacridar (100 mg/kg, p.o.) and crizotinib increases the plasma and brain concentrations and brain-to-plasma ratios of crizotinib in wild-type mice, 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 elacridar 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, elacridar fully inhibits P-gp mediated transport of topotecan, 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 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 3.0×103 cells per well are seeded in a 96-well plate. After 24 h incubation, an optimum concentration gradient of elacridar is added to each well. After culturing for 48 h, 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.

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：

Ritonavir reverses resistance to docetaxel and cabazitaxel in prostate cancer cells with acquired resistance to docetaxel [ Cancer Drug Resist, 2024, 7:3] PubMed: 38318527
Abcg2a is the functional homolog of human ABCG2 expressed at the zebrafish blood-brain barrier [ bioRxiv, 2023, 10.1101/2023.05.18.539313] PubMed: 37425689
Abcg2a is the functional homolog of human ABCG2 expressed at the zebrafish blood-brain barrier [ bioRxiv, 2023, 2023.05.18.539313] PubMed: 37425689
Activation of STAT3 through combined SRC and EGFR signaling drives resistance to a mitotic kinesin inhibitor in glioblastoma [ Cell Rep, 2022, 39(12):110991] PubMed: 35732128
Overcoming Resistance to Anti–Nectin-4 Antibody-Drug Conjugate [ Mol Cancer Ther, 2022, 21 (7): 1227–1235.] PubMed: None
Overcoming Resistance to Anti-nectin-4 Antibody-Drug Conjugate [ Mol Cancer Ther, 2022, molcanther.0013.2022] PubMed: 35534238
ETV7 regulates breast cancer stem-like cell features by repressing IFN-response genes [ Cell Death Dis, 2021, 12(8):742] PubMed: 34315857
Estradiol regulates intestinal ABCG2 to promote urate excretion via the PI3K/Akt pathway [ Nutr Metab (Lond), 2021, 18(1):63] PubMed: 34144706
Therapeutic Targeting of MDR1 Expression by RORγ Antagonists Resensitizes Cross-Resistant CRPC to Taxane via Coordinated Induction of Cell Death Programs. [ Mol Cancer Ther, 2020, 19(2):364-374] PubMed: 31712394
Multiple ABCB1 transcriptional fusions in drug resistant high-grade serous ovarian and breast cancer. [ Nat Commun, 2019, 10(1):1295] PubMed: 30894541

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。