Limantrafin (CB-103)

製品コードS9719 バッチS971901

印刷

化学情報

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

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	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 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。	2.400mg/ml (9.90mM)	Taking the 1 mL working solution as an example, add 50 μL of 48 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil 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。	2.400mg/ml (9.90mM)	Taking the 1 mL working solution as an example, add 50 μL of 48 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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	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	Limantrafin (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	Limantrafin (CB-103) function in vivo recapitulates genetic notch loss-of-function phenotypes without causing gut toxicity, and it 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. Limantrafin (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

参考

https://pubmed.ncbi.nlm.nih.gov/32601208/

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：

Notch1 Phase Separation Coupled Percolation facilitates target gene expression and enhancer looping [ Sci Rep, 2024, 14(1):21912]	PubMed: 39300145
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。