Selinexor (KPT-330)

製品コードS7252 バッチS725203

印刷

化学情報

Chemical Structure Synonyms ATG-010 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H11F6N7O
分子量 443.31 CAS No. 1393477-72-9
Solubility (25°C)* 体外 DMSO 88 mg/mL (198.5 mM)
Ethanol 88 mg/mL (198.5 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Selinexor (KPT-330, ATG-010) is an orally bioavailable selective CRM1 inhibitor. Phase 2.
in vitro As the clinical candidate analog of KPT-185, KPT-330 exhibits similar effects on the viability of T-ALL cells and elicits rapid apoptotic response. KPT-330 also reduces cell growth in MOLT-4, Jurkat, HBP-ALL, KOPTK-1, SKW-3, and DND-41 cell lines, with IC50 values of 34-203 nM. [1]
in vivo KPT-330 dramatically suppresses the growth of T-ALL cells (MOLT-4) and AML cells (MV4–11) in vivo, with little toxicity to normal haematopoietic cells. [1] In SCID mice with diffuse human MM bone lesions, KPT-330 inhibits MM-induced bone lysis and prolongs survival. Moreover, KPT-330 directly impairs osteoclastogenesis and bone resorption by blocking RANKL-induced NF-κB and NFATc1, with minimal impact on osteoblasts and BMSCs. [2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MOLT-4, Jurkat, HBP-ALL, KOPTK-1, SKW-3, and DND-41 cell lines
濃度 ~1 μM
反応時間 72 hours
実験の流れ Cell lines are cultured in RPMI 1640 medium, supplemented with 10% fetal bovine serum and penicillin/streptomycin. Cell Titer Glo assay is used to assess cell viability upon treatment with either dimethyl sulfoxide (DMSO) or KPT-330. Cells are plated at a density of 10 000 cells per well in a 96-well plate and incubated with DMSO or increasing concentrations of KPT-330. The cell viability is measured after 72 h exposure to KPT-330 and reported as a percentage of DMSO control cells. Jurkat cells that overexpress BCL2 are generated using MSCV-IRES-GFP retroviral expression system. Jurkat cells infected with BCL2 or control vector viruses are sorted by flow cytometry and the expression of BCL2 confirmed by Western blot analysis using BCL2 antibody.
動物実験 動物モデル T-ALL and AML orthograft mouse model
投薬量 20 -25 mg/kg
投与方法 p.o.

カスタマーフィードバック

, , Mol Cancer Ther, 2017, 16(4):717-728

Data from [Data independently produced by , , J Cell Mol Med, 2018, doi:10.1111/jcmm.13886]

Data from [Data independently produced by , , BMC Cancer, 2018, 18(1):764]

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
p300 nucleocytoplasmic shuttling underlies mTORC1 hyperactivation in Hutchinson-Gilford progeria syndrome [ Nat Cell Biol, 2024, 10.1038/s41556-023-01338-y] PubMed: 38267537
Cold-induced FOXO1 nuclear transport aids cold survival and tissue storage [ Nat Commun, 2024, 15(1):2859] PubMed: 38570500
Androgen deprivation induces double-null prostate cancer via aberrant nuclear export and ribosomal biogenesis through HGF and Wnt activation [ Nat Commun, 2024, 15(1):1231] PubMed: 38336745
UCHL1 is a potential molecular indicator and therapeutic target for neuroendocrine carcinomas [ Cell Rep Med, 2024, S2666-3791(23)00610-9] PubMed: 38244540
A first-in-class inhibitor of HSP110 to potentiate XPO1-targeted therapy in primary mediastinal B-cell lymphoma and classical Hodgkin lymphoma [ J Exp Clin Cancer Res, 2024, 43(1):148] PubMed: 38773631
A first-in-class inhibitor of HSP110 to potentiate XPO1-targeted therapy in primary mediastinal B-cell lymphoma and classical Hodgkin lymphoma [ J Exp Clin Cancer Res, 2024, 43(1):148] PubMed: 38773631
A common druggable signature of oncogenic c-Myc, mutant KRAS and mutant p53 reveals functional redundancy and competition among oncogenes in cancer [ Cell Death Dis, 2024, 15(8):638] PubMed: 39217152
Dihydrolipoamide dehydrogenase (DLD) is a novel molecular target of bortezomib [ Cell Death Dis, 2024, 15(8):588] PubMed: 39138149
Targeting TRIP13 in favorable histology Wilms tumor with nuclear export inhibitors synergizes with doxorubicin [ Commun Biol, 2024, 7(1):426] PubMed: 38589567

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。