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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 | C16H10F8N4O |
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分子量 | 426.26 | CAS No. | 1421919-75-6 | ||||
Solubility (25°C)* | 体外 | DMSO | 20 mg/mL (46.91 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. |
製品説明 | KPT-276 is an orally bioavailable selective CRM1 inhibitor. |
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in vitro | KPT-276 results in significant growth inhibition and apoptosis induction in MCL cells. [2] KPT-276 specifically and irreversibly inhibits the nuclear export function of XPO1, and reduces the viability of 12 HMCLs. KPT-276 also actively induces apoptosis in primary MM patient samples. [3] |
in vivo | KPT-276 significantly prolongs survival of leukemic mice and reduces leukemic burden in a xenograft AML mouse model. [1] KPT-276 significantly suppresses tumor growth in an MCL-bearing severe combined immunodeficient mouse model without severe toxicity. [2] KPT-276 reduces monoclonal spikes in the Vk*MYC transgenic MM mouse model, and inhibits tumor growth in a xenograft MM mouse model. [3] |
特徴 | Superior oral bioavailability and PK profile relative to KPT-185 in vivo. Potential for use in hematological malignancies such as AML and multiple myeloma. |
動物実験 | 動物モデル | Human leukemia (MV4-11) xenografts are established in mice. |
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投薬量 | ~150 mg/kg | |
投与方法 | Oral gavage |
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Traumatic injury compromises nucleocytoplasmic transport and leads to TDP-43 pathology [ Elife, 2021, 10e67587] | PubMed: 34060470 |
Transcriptome Profiling of Acquired Gefitinib Resistant Lung Cancer Cells Reveals Dramatically Changed Transcription Programs and New Treatment Targets [ Front Oncol, 2020, 10:1424] | PubMed: 32923394 |
Modulation of actin polymerization affects nucleocytoplasmic transport in multiple forms of amyotrophic lateral sclerosis. [ Nat Commun, 2019, 10(1):3827] | PubMed: 31444357 |
The C9orf72 repeat expansion disrupts nucleocytoplasmic transport [Zhang K Nature, 2015, 525(7567):56-61] | PubMed: 26308891 |
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。