Limantrafin (CB-103)

製品コードS9719 バッチS971901

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C15H18N2O
分子量 242.32 CAS No. 218457-67-1
Solubility (25°C)* 体外 DMSO 48 mg/mL (198.08 mM)
Ethanol 48 mg/mL (198.08 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

Limantrafin (CB-103) is an orally active inhibitor of the Notch transcription activation complex. CB-103 produces Notch loss-of-function phenotypes in flies and mice and inhibits the growth of human breast cancer and leukemia xenografts.
in vitro

CB-103 inhibits growth of Notch-addicted human T cell acute lymphoblastic leukemia cell lines through modulation of the Notch transcription complex.[1]
in vivo

CB-103 function in vivo recapitulates genetic notch loss-of-function phenotypes without causing gut toxicity. CB-103 blocks tumor growth of GSI-resistant cancers.[1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 marrow mesenchymal stroma cells (MSCs), RPMI-8402 cells
濃度 10 nM to 25 μM, 1 μM
反応時間 3 days, 1 h, 4 h, 24 h
実験の流れ

MSCs are seeded in 384-well plates at a concentration of 2,500 cells per well in 30 μL AIMV medium. After 24 hours, ALL cells are added at a concentration of 25,000 to 30,000 cells per well in 27.5 μL AIMV. CB-103 or DMSO as control is added after an additional 24 hours at five different concentrations (from 10 nM to 25 μM). Three days later, ALL cells are collected from cocultures by scraping and stained with 7-AAD. Cell viability is measured by flow cytometry using counting beads for cell count normalization.
動物実験 動物モデル NOD/SCIDγc-/- mice, C57Bl/6 wt mice
投薬量 20 mg/kg, 25 mg/kg
投与方法 Oral gavage

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：

Familial Alzheimer's disease-associated PSEN1 mutations affect neurodevelopment through increased Notch signaling [ Stem Cell Reports, 2023, 18(7):1516-1533] PubMed: 37352850
Evaluation of the anticancer activity of RIN-1, a Notch signaling modulator, in head and neck squamous cell carcinoma [ Sci Rep, 2023, 13(1):13700] PubMed: 37607974
Evaluation of the anticancer activity of RIN-1, a Notch signaling modulator, in head and neck squamous cell carcinoma [ Sci Rep, 2023, 13(1):13700] PubMed: 37607974
GALNT2 promotes cell proliferation, migration, and invasion by activating the Notch/Hes1-PTEN-PI3K/Akt signaling pathway in lung adenocarcinoma [ Life Sci, 2021, 276:119439] PubMed: 33785338

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。