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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C16H13BrF3IN2O4 |
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分子量 | 561.09 | CAS No. | 391210-00-7 | |
Solubility (25°C)* | 体外 | DMSO | 112 mg/mL (199.61 mM) | |
Ethanol | 14 mg/mL (24.95 mM) | |||
Water | 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. |
製品説明 | PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. |
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in vitro | PD318088 is a small-molecule inhibitor of MEK1/2, which is an analog of PD184352, suggesting it might have substantial anti-proliferative activity against cancer cells, although no functional study of PD318088 is currently available. PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. Formation of the ternary complexes with PD318088 and MgATP results in moderate increases (to 140 nM) for the Kd monomer-dimer for both MEK1 and MEK2. The binding of PD318088 and MgATP to MEK1 also abolishes the formation of tetramers and higher-order aggregates. PD318088 and MgATP together increase the dimerization disassociation constant for MEK1 and MEK2 slightly from ~75 nM to ~140 nM, suggesting that the mechanism of inhibition for PD318088 is probably a result of localized conformational changes in the active site and not a global change in the overall structure. [1] |
, , Dr. Zhang of Tianjin Medical University
Comprehensive drug response profiling and pan-omic analysis identified therapeutic candidates and prognostic biomarkers for Asian cholangiocarcinoma [ iScience, 2022, 25(10):105182] | PubMed: 36248745 |
Identification of New Vulnerabilities in Conjunctival Melanoma Using Image-Based High Content Drug Screening [ Cancers (Basel), 2022, 14(6)1575] | PubMed: 35326726 |
CAGE-prox: A Unified Approach for Time-Resolved Protein Activation in Living Systems [ Curr Protoc, 2021, 1(6):e180] | PubMed: 34165886 |
Time-resolved protein activation by proximal decaging in living systems [Wang J, et al. Nature, 2019, 569(7757):509-513] | PubMed: 31068699 |
MEK inhibitors activate Wnt signalling and induce stem cell plasticity in colorectal cancer [ Nat Commun, 2019, 10(1):2197] | PubMed: 31097693 |
DRUGPATH - a novel bioinformatic approach identifies DNA-damage pathway as a regulator of size maintenance in human ESCs and iPSCs [ Sci Rep, 2019, 9(1):1897] | PubMed: 30760778 |
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。