SR18662

製品コードS8900 バッチS890001

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

C16H19Cl2N3O4S

分子量 420.31 CAS No. 2505001-62-5
Solubility (25°C)* 体外 DMSO 84 mg/mL (199.85 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)
Clear solution
5% DMSO 95% corn oil
0.35mg/ml Taking the 1 mL working solution as an example, add 50 μL of 7 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. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.4mg/ml Taking the 1 mL working solution as an example, add 50 μL of clarified DMSO stock solution of 28 mg/ml to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; 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. 
* <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 SR18662 is an optimized compund based on ML264 that inhibits Krüppel-like factor 5 (KLF5) with IC50 of 4.4 nM. SR18662 reduces the viability of multiple colorectal cancer cell lines. SR18662 induces apoptosis.
in vitro

Treatment with SR18662 significantly reduces growth and proliferation of CRC cells. SR18662 shows improved efficacy in reducing viability of multiple CRC cell lines. Flow cytometry analysis following SR18662 treatment shows an increase in cells captured in either S or G2/M phases of the cell cycle and a significant increase in the number of apoptotic cells. SR18662 treatment also reduces the expression of cyclins and components of MAPK and WNT signaling pathways.[1]

in vivo

A significant dose-dependent inhibition of xenograft growth in mice is observed following SR18662 treatment that exceeds the effect of ML264 at equivalent doses. SR18662 is potential for colorectal cancer therapy.[1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 DLD-1, HCT116, HT29 and SW620 colorectal cancer cell lines
濃度 0.001 μM-20 μM
反応時間 24 h
実験の流れ

KLF5 promoter activity assay: DLD-1/pGL4.18hKLF5p cells are seeded in 96 well plate format and treated with DMSO or with SR18662 dissolved in DMSO in the range of 0.001 to 20 μM final concentration for 24 h and the human KLF5 promoter activity is determined with the ONE-Glo luciferase assay system using a SpectramMax M3 plate reader.

動物実験 動物モデル 7-week-old male NuJ/Foxn1nu mice with DLD-1 human colorectal cells injected
投薬量 5 mg/kg, 10 mg/kg, 25 mg/kg
投与方法 IP

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:

Inhibiting the glycerophosphodiesterase EDI3 in ER-HER2+ breast cancer cells resistant to HER2-targeted therapy reduces viability and tumour growth [ J Exp Clin Cancer Res, 2023, 42(1):25] PubMed: 36670508

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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