Selinexor (KPT-330)

製品コードS7252 バッチS725208

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 89 mg/mL (200.76 mM)
Ethanol 22 mg/mL (49.62 mM)
Water 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.
* <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, Selinexor (KPT-330) exhibits similar effects on the viability of T-ALL cells and elicits rapid apoptotic response. It 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 Selinexor (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, it inhibits MM-induced bone lysis and prolongs survival. Moreover, this compound 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 Selinexor (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 this compound. The cell viability is measured after 72 h exposure to it 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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/23373539/
  • https://pubmed.ncbi.nlm.nih.gov/23588715/

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：

Disparate leukemia mutations converge on nuclear phase-separated condensates [ Cell, 2025, S0092-8674(25)01149-3] PubMed: 41192422
Human iPSC-derived nephron progenitor cells treat acute kidney injury and chronic kidney disease in mouse models [ Sci Transl Med, 2025, 17(792):eadt5553] PubMed: 40173262
The macrophage-intrinsic MDA5/IRF5 axis drives HIV-1 intron-containing RNA-induced inflammatory responses [ J Clin Invest, 2025, 135(16)e187663] PubMed: 40493408
Nuclear to Cytoplasmic Transport Is a Druggable Dependency in HDAC7-driven Small Cell Lung Cancer [ Adv Sci (Weinh), 2025, 12(14):e2413445] PubMed: 39887933
A patient-derived T cell lymphoma biorepository uncovers pathogenetic mechanisms and host-related therapeutic vulnerabilities [ Cell Rep Med, 2025, S2666-3791(25)00102-8] PubMed: 40147445
Nuclear paxillin functions as a molecular switch for alternative splicing in neurons during a critical period of brain development [ EMBO J, 2025, 44(21):5965-5992] PubMed: 40926123
NPM1-fusion proteins promote myeloid leukemogenesis through XPO1-dependent HOX activation [ Leukemia, 2025, 39(1):75-86] PubMed: 39443736
Atovaquone and selinexor as a novel combination treatment option in acute myeloid leukemia [ Cancer Lett, 2025, 613:217501] PubMed: 39864539
Targeting fucosyltransferase FUT8 as a prospective therapeutic approach for DLBCL [ Oncogenesis, 2025, 14(1):1] PubMed: 39881135
Regulation of chromatin modifications through coordination of nucleus size and epithelial cell morphology heterogeneity [ Commun Biol, 2025, 8(1):269] PubMed: 39979587

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。

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