KPT-276

製品コードS7251 バッチS725101

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₆H₁₀F₈N₄O

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）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%PEG400 1 0.5%Tween80 2 5%propylene glycol この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (11.73mM)	Taking the 1 mL working solution as an example, add 300 μL of 16.67 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O Dilute to 1 mL. The mixed solution should be used immediately for optimal results.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	KPT-276は経口バイオアベイラブルな選択的CRM1阻害剤です。
in vitro	KPT-276 results in significant growth inhibition and apoptosis induction in MCL cells. This compound specifically and irreversibly inhibits the nuclear export function of XPO1, and reduces the viability of 12 HMCLs. It also actively induces apoptosis in primary MM patient samples.
in vivo	KPT-276 significantly prolongs survival of leukemic mice and reduces leukemic burden in a xenograft AML mouse model. This compound significantly suppresses tumor growth in an MCL-bearing severe combined immunodeficient mouse model without severe toxicity. It reduces monoclonal spikes in the Vk*MYC transgenic MM mouse model, and inhibits tumor growth in a xenograft MM mouse model.
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.

プロトコル(参考用のみ)

動物実験	動物モデル	Human leukemia (MV4-11) xenografts are established in mice.
	投薬量	~150 mg/kg
	投与方法	Oral gavage

参考

https://pubmed.ncbi.nlm.nih.gov/22677130/
https://pubmed.ncbi.nlm.nih.gov/22986101/
https://pubmed.ncbi.nlm.nih.gov/23752175/

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：

Inhibition of XPO1 by selinexor enhances terminal erythroid maturation through modulation of HSP70 trafficking in severe β0-thalassemia/HbE [ PLoS One, 2025, 20(9):e0333127]	PubMed: 40997022
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。