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化学情報
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Synonyms | CGP-72670, ICL-670 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C21H15N3O4 |
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| 分子量 | 373.36 | CAS No. | 201530-41-8 | |
| Solubility (25°C)* | 体外 | DMSO | 74 mg/mL (198.2 mM) | |
| Ethanol | 15 mg/mL (40.17 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 | Deferasirox is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor. Deferasirox-induced iron depletion promotes BclxL downregulation and cell death. |
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| in vitro | Deferasirox effectively chelates iron from Rhizopus oryzae and demonstrates cidal activity in vitro against 28 of 29 clinical isolates of Mucorales at concentrations well below clinically achievable serum levels. [1] Deferasirox incubation induces a significant inhibition of NF-κB activity and a cytoplasmic sequestration of its active subunit p65 in an inactive form in 28 of 40 peripheral blood samples. [2] Deferasirox inhibits three human myeloid cell lines (K562, U937, and HL60) with IC50 of 17-50 mM. [3] Deferasirox is cidal in vitro against A. fumigatus, with an MIC and MFC of 25 and 50 mg/L, respectively. [5] |
| in vivo | Deferasirox significantly improves survival and decreased tissue fungal burden in diabetic ketoacidotic or neutropenic mice with mucormycosis, with an efficacy similar to that of liposomal amphotericin B. Deferasirox treatment also enhances the host inflammatory response to mucormycosis. Deferasirox synergistically improves survival and reduces tissue fungal burden when combined with liposomal amphotericin B. [1] Deferasirox administered p.o. to rats is absorbed to at least 75%, and the bioavailability is 26%.Deferasirox is present in the blood circulation mainly in the unchanged form and as its iron complex, Fe(deferasirox)2, after intravenous and p.o. administration. Deferasirox is 99.2% bound to plasma proteins. [4] Deferasirox monotherapy modestly prolongs survival of mice with IPA. [5] |
プロトコル(参考用のみ)
参考
カスタマーフィードバック
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, , Nature, 2014, 509(7498):105-9.
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：
| Overburdened ferroptotic stress impairs tooth morphogenesis [ Elife, 2023, 12RP88745] | PubMed: 37991825 |
| β-catenin-IRP2-primed iron availability to mitochondrial metabolism is druggable for active β-catenin-mediated cancer [ J Transl Med, 2023, 21(1):50] | PubMed: 36703130 |
| Dihydroartemisinin-induced ferroptosis in acute myeloid leukemia: links to iron metabolism and metallothionein [ Cell Death Discov, 2023, 9(1):97] | PubMed: 36928207 |
| NCOA4-Mediated Ferritinophagy Is a Pancreatic Cancer Dependency via Maintenance of Iron Bioavailability for Iron-Sulfur Cluster Proteins [ Cancer Discov, 2022, 12(9):2180-2197] | PubMed: 35771492 |
| Targeting cellular iron homeostasis with ironomycin in diffuse large B cell lymphoma [ Cancer Res, 2022, canres.0218.2021] | PubMed: 35078814 |
| Downregulation of hepatic ceruloplasmin ameliorates NAFLD via SCO1-AMPK-LKB1 complex [ Cell Rep, 2022, 41(3):111498] | PubMed: 36261001 |
| Iron chelator deferasirox inhibits NF-κB activity in hepatoma cells and changes sorafenib-induced programmed cell deaths [ Biomed Pharmacother, 2022, 153:113363] | PubMed: 35834989 |
| Tumor cell-imposed iron restriction drives immunosuppressive polarization of tumor-associated macrophages [ J Transl Med, 2021, 19(1):347] | PubMed: 34389031 |
| Deferasirox induces cyclin D1 degradation and apoptosis in mantle cell lymphoma in a reactive oxygen species- and GSK3β-dependent mechanism [ Br J Haematol, 2021, 192(4):747-760] | PubMed: 33521925 |
| Deferasirox-Dependent Iron Chelation Enhances Mitochondrial Dysfunction and Restores p53 Signaling by Stabilization of p53 Family Members in Leukemic Cells [ Int J Mol Sci, 2020, 21(20)E7674] | PubMed: 33081324 |
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。