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受注：045-509-1970 |
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化学情報
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Synonyms | MK 8628 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C25H22ClN5O2S |
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| 分子量 | 491.99 | CAS No. | 202590-98-5 | |
| Solubility (25°C)* | 体外 | DMSO | 98 mg/mL (199.19 mM) | |
| Ethanol | 98 mg/mL (199.19 mM) | |||
| Water | Insoluble | |||
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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 | Birabresib (OTX015, MK 8628) is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Birabresib inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. |
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| in vitro | OTX015 inhibits the binding of BRD2, BRD3, and BRD4 to AcH4 with IC50 ranging from 92 to 112 nM, and inhibits the growth of a variety of human cancer cell lines with GI50 ranging from 60 to 200 nM. [1] OTX015 results in rapid down-regulation of c-MYC expression, and show the synergistic anti-proliferative effects in combination with ALK inhibitors in ALKpos ALCL cell lines. [2] |
| in vivo | OTX015 (p.o.) significantly inhibits the growth of Ty82 BRD-NUT midline carcinoma tumors in nude mice by 79% at 100 mg/kg qd and 61% at 10 mg/kg bid, respectively. [1] |
| 特徴 | Orally bioavailable BRD2/3/4-selective inhibitor that has been tested in Phase I clinical trials for treatment of Haematological Malignancies. |
プロトコル(参考用のみ)
| キナーゼアッセイ | TR-FRET Assay [1] | |
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| To assess binding of OTX015 to BRD2, BRD3, and BRD4, BRD-expressing CHO cell lysate (from CHO cells transfected with expression plasmids for Flag-tagged BRD2, BRD3, or BRD4 or vector alone), europium-conjugated anti-Flag antibody, XL-665-conjugated streptavidin, and biotinylated OTX015 are incubated at room temperature for 0.2 to 2 h. Fluorescence is measured by TR-FRET using an EnVision 2103 Multilabel Reader and EC50 for binding is calculated by nonlinear regression using PRISM version 5.02. | ||
| 細胞アッセイ | 細胞株 | Human tumor cells |
| 濃度 | ~2 μM | |
| 反応時間 | 72 hours | |
| 実験の流れ | Effects of OTX015 on cancer cell proliferation are evaluated by incubating human tumor cells for 72 h with increasing concentrations of OTX015 and assessing proliferation using a tetrazolium salt (WST-8)-based colorimetric assay. |
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| 動物実験 | 動物モデル | BLAB/c-nu/nu mice bearing established Ty82 BRD-NUT midline carcinoma xenografts. |
| 投薬量 | ~100 mg/kg | |
| 投与方法 | p.o. | |
参考
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カスタマーフィードバック
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, , Mol Cancer Ther, 2016, 16(4 suppl 1):S263-S276
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Data from [Data independently produced by , , Clin Cancer Res, 2018, 24(16):3941-3954]
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Data from [Data independently produced by , , Clin Cancer Res, 2018, doi: 10.1158/1078-0432.CCR-18-1040]
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：
| Dual Inhibition of CDK4/6 and XPO1 Induces Senescence With Acquired Vulnerability to CRBN-Based PROTAC Drugs [ Gastroenterology, 2024, S0016-5085(24)00062-3] | PubMed: 38262581 |
| RAPID resistance to BET inhibitors is mediated by FGFR1 in glioblastoma [ Sci Rep, 2024, 14(1):9284] | PubMed: 38654040 |
| HNF4α, SP1 and c-myc are master regulators of CNS autoimmunity [ J Autoimmun, 2023, 138:103053] | PubMed: 37236124 |
| "Proteotranscriptomic analysis of advanced colorectal cancer patient derived organoids for drug sensitivity prediction" [ J Exp Clin Cancer Res, 2023, 42(1):8] | PubMed: 36604765 |
| Combination drug screen targeting glioblastoma core vulnerabilities reveals pharmacological synergisms [ EBioMedicine, 2023, 95:104752] | PubMed: 37572644 |
| Combination drug screen targeting glioblastoma core vulnerabilities reveals pharmacological synergisms [ EBioMedicine, 2023, 95:104752] | PubMed: 37572644 |
| Pharmacological inhibition of bromodomain and extra-terminal proteins induces an NRF-2-mediated antiviral state that is subverted by SARS-CoV-2 infection [ PLoS Pathog, 2023, 19(9):e1011657] | PubMed: 37747932 |
| ACC010, a novel BRD4 inhibitor, synergized with homoharringtonine in acute myeloid leukemia with FLT3-ITD [ Mol Oncol, 2023, 17(7):1402-1418] | PubMed: 36567628 |
| Epigenetic Regulation of MAP3K8 in EBV-Associated Gastric Carcinoma [ Int J Mol Sci, 2023, 24(3)1964] | PubMed: 36768307 |
| XIST loss impairs mammary stem cell differentiation and increases tumorigenicity through Mediator hyperactivation [ Cell, 2022, S0092-8674(22)00532-3] | PubMed: 35597241 |
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。