compound 3i (666-15)

製品コードS8846 バッチS884601

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

C33H31Cl2N3O5
分子量 620.52 CAS No. 1433286-70-4
Solubility (25°C)* 体外 DMSO 100 mg/mL (161.15 mM)
Ethanol 3 mg/mL (4.83 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml
5% DMSO 95% Corn oil
2.5mg/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 Compound 3i (666-15) is a potent and selective inhibitor of CREB-mediated gene transcription (IC50 = 0.081 ± 0.04 μM) and also potently inhibits cancer cell growth without harming normal cells.
in vitro

666-15 could potently inhibit cancer cell growth. In MDA-MB-231 and MDA-MB-468 cells, the GI50 for 666-15 is 73 and 46 nM, respectively. In A549 and MCF-7 cells, it exhibit robust activity as well with GI50 of 0.47 and 0.31 μM. 666-15 inhibits CREB’s transcription activity in living cells independent of direct CREB or CBP binding interaction[1].
in vivo

In an in vivo MDA-MB-468 xenograft model, 666-15 completely suppresses the tumor growth without overt toxicity. Preliminary toxicity studies show that intraperitoneal (ip) injection of 10 mg/kg of 666-15 is well tolerated in mice[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HEK 293T cells
濃度 0.05, 0.1, 0.5 μM
反応時間 --
実験の流れ

HEK 293T cells are treated with different concentrations of 666-15 followed by treatment with forskolin. Then the relative mRNA level of Nurr1/NR4A2 is determined by qRT-PCR analysis.
動物実験 動物モデル 6- to 8-week old BALB/c nude mouse inoculated subcutaneously at the right flank with MDA-MB-468 cells
投薬量 10 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：

The delta subunit of the GABAA receptor is necessary for the GPT2-promoted breast cancer metastasis [ Theranostics, 2023, 13(4):1355-1369] PubMed: 36923530
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
MLK4 promotes glucose metabolism in lung adenocarcinoma through CREB-mediated activation of phosphoenolpyruvate carboxykinase and is regulated by KLF5 [ Oncogenesis, 2023, 12(1):35] PubMed: 37407566
MLK4 promotes glucose metabolism in lung adenocarcinoma through CREB-mediated activation of phosphoenolpyruvate carboxykinase and is regulated by KLF5 [ Oncogenesis, 2023, 12(1):35] PubMed: 37407566
Paradoxical Induction of ALOX15/15B by Cortisol in Human Amnion Fibroblasts: Implications for Inflammatory Responses of the Fetal Membranes at Parturition [ Int J Mol Sci, 2023, 24(13)10881] PubMed: 37446059
LIM1 contributes to the malignant potential of endometrial cancer [ Front Oncol, 2023, 13:1082441] PubMed: 36969081
pH sensing controls tissue inflammation by modulating cellular metabolism and endo-lysosomal function of immune cells [ Nat Immunol, 2022, 10.1038/s41590-022-01231-0] PubMed: 35668320
Downregulation of IL-8 and IL-10 by the Activation of Ca2+-Activated K+ Channel KCa3.1 in THP-1-Derived M2 Macrophages [ Int J Mol Sci, 2022, 23(15)8603] PubMed: 35955737
Activation of cAMP Signaling in Response to α-Phellandrene Promotes Vascular Endothelial Growth Factor Levels and Proliferation in Human Dermal Papilla Cells [ Int J Mol Sci, 2022, 23(16)8959] PubMed: 36012223
Gab2 promotes acute myeloid leukemia growth and migration through the SHP2-Erk-CREB signaling pathway [ J Leukoc Biol, 2022, 10.1002/JLB.2A0421-221R] PubMed: 35322464

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。