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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 | ARRY-142886 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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| 化学式 | C17H15BrClFN4O3 |
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| 分子量 | 457.68 | CAS No. | 606143-52-6 | ||||
| Solubility (25°C)* | 体外 | DMSO (warmed with 50ºC water bath) | 91 mg/mL (198.82 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） |
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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 | Selumetinib (AZD6244, ARRY-142886) is a potent, highly selective MEK inhibitor with IC50 of 14 nM for MEK1 and Kd value of 530 nM for MEK2. It also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Selumetinib suppresses cell proliferation, migration and trigger apoptosis. Phase 3. |
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| in vitro | Selumetinib (AZD6244) is not competitive with ATP and inactivates the ERK1/2 phosphorylation with IC50 concentrations below 40 nM. It also inhibits the growth of primary HCC cells through inhibition of ERK1/2 and p90RSK phosphorylation, accompanied with elevation of the cleavage of caspase-3 and caspase-7, and cleaved poly(ADP)ribose polymerase. This compound has little effects on the p38, c-Jun-NH2-kinase, phosphatidylinositol 3-kinase, and MEK5/ERK5 pathways. [1] It is sensitive to Raf mutations in breast cancer cell lines and Ras mutations in NSCLC cell lines. [2] |
| in vivo | Selumetinib (AZD6244) significantly inhibits phosphorylation of ERK1/2 in 2-1318, 5-1318, 26-1004 and 4-1318 xenografts and induces apoptosis in primary 2-1318 cells by activating the caspase pathway. [1] It could inhibit the tumor growth in HT-29 xenograft, which is a colorectal tumor model carrying a B-Raf mutation, at a dose of 100 mg/kg and the tumor growth inhibition of this compound is better. [3] Otherwise it could inhibit HCC xenografts tumor growth, which associated with increased apoptosis and down-regulation of cell cycle regulators, including cyclin D1, Cdc-2, CDK2 and 4, cyclin B1, and c-Myc. [4] |
| 特徴 | First MEK inhibitor being tested in Phase II clinical trials. |
プロトコル(参考用のみ)
| キナーゼアッセイ | Assay of MEK Kinase Activity | |
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| Selumetinib (AZD6244) is used to immunoprecipitate MEK1 molecules. MEK kinase activity is measured as the ability of immuno-isolated MEK1 to activate recombinant ERK1 in a coupled assay using MBP as the end point of the assay. Phosphorylated MBP is resolved on a 14% SDS-PAGE gel and vacuum-dried before exposure to X-ray film. | ||
| 細胞アッセイ | 細胞株 | Primary HCC cell lines including 2-1318, 4-1318 and 26-1004 cells |
| 濃度 | ~ 10 μM | |
| 反応時間 | 24 or 48 hours | |
| 実験の流れ | After seeding cells at a density of 2.0 × 104 and 48 hours of incubation, they are rinsed twice with culture media. Selumetinib (AZD6244) is then used to treat the cells at various concentrations for 24 or 48 hours. Cell viability is determined by the 3-(4,5-dimethylthiazol-2y1)-2,5-diphenyltetrazolium bromide (MTT) assay. Cell proliferation is assayed using a bromodeoxyuridine kit. |
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| 動物実験 | 動物モデル | HCC xenografts in mice homozygous for the SCID (severe combined immunodeficiency) mutation |
| 投薬量 | 50 or 100mg/kg | |
| 投与方法 | Administered via p.o. | |
参考
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カスタマーフィードバック
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Data from [Oncogene, 2012, 31, 3277–3286]
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Data from [Nature, 2010, 468, 968-972]
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Data from [Nature, 2010, 468, 973-977]
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：
| A patient-derived T cell lymphoma biorepository uncovers pathogenetic mechanisms and host-related therapeutic vulnerabilities [ Cell Rep Med, 2025, S2666-3791(25)00102-8] | PubMed: 40147445 |
| GCLM lactylation mediated by ACAT2 promotes ferroptosis resistance in KRASG12D-mutant cancer [ Cell Rep, 2025, 44(6):115774] | PubMed: 40503938 |
| Targeting LINC02320 prevents colorectal cancer growth via GRB7-dependent inhibition of MAPK signaling pathway [ Cell Mol Biol Lett, 2025, 30(1):86] | PubMed: 40691533 |
| Methylstat sensitizes ovarian cancer cells to PARP-inhibition by targeting the histone demethylases JMJD1B/C [ Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z] | PubMed: 39915607 |
| Basroparib overcomes acquired resistance to MEK inhibitors by inhibiting Wnt-mediated cancer stemness in KRAS-mutated colorectal cancer [ Biochem Pharmacol, 2025, 235:116842] | PubMed: 40024348 |
| Secreted Cytokines From Inflammatory Macrophages Modulate Sex Differences in Valvular Interstitial Cells on Hydrogel Biomaterials [ J Biomed Mater Res A, 2025, 113(3):e37885] | PubMed: 39995146 |
| Acquired resistance to vemurafenib restrains thyroid cancer stem cell self-renewal by suppressing STAT3 activation [ Cell Signal, 2025, 133:111845] | PubMed: 40345509 |
| Tumour-selective activity of RAS-GTP inhibition in pancreatic cancer [ Nature, 2024, 629(8013):927-936] | PubMed: 38588697 |
| SHANK3 depletion leads to ERK signalling overdose and cell death in KRAS-mutant cancers [ Nat Commun, 2024, 15(1):8002] | PubMed: 39266533 |
| SRF SUMOylation modulates smooth muscle phenotypic switch and vascular remodeling [ Nat Commun, 2024, 15(1):6919] | PubMed: 39134547 |
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。