MYCi975

製品コードS8906 バッチS890602

印刷

化学情報

Chemical Structure Synonyms NUCC-0200975 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C25H16Cl2F6N2O2
分子量 561.30 CAS No. 2289691-01-4
Solubility (25°C)* 体外 DMSO 100 mg/mL (178.15 mM)
Ethanol 100 mg/mL (178.15 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 MYCi975 (NUCC-0200975) is a potent, selective and orally active inhibitor of MYC that disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression. MYCi975 exhibits potent anti-tumor activities.

生物活性

製品説明 MYCi975 (NUCC-0200975) is a potent, selective and orally active inhibitor of MYC that disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression. MYCi975 exhibits potent anti-tumor activities.
in vitro

MYCi975 localizes to the same region of the MYC protei. Treatment of cells with MYCi975 enhances MYC degradation and phosphorylation on T58. MYCi975 also directly increases GSK3b-mediated MYC pT58 in the in vitro kinase assay.[1]
in vivo

MYCi975 suppresses in vivo tumor growth in mice, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy with good tolerability.[1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MycCaP, PC3, LNCaP, PC12, MV411, SK-N-BE (2), 293T, P493-6 B cells, LLC1 cells, TGR-1, HO15.19 Rat-1 cells
濃度 3-25 μM, 8 μM, 6 μM
反応時間 24 h
実験の流れ

PC3 cells are treated with 6 μM 361 or 8 μM 975 and P493-6 cells are treated with 0.1 mg/ml Tetracycline or 6 μM 975 for 24 hr in triplicates. Then cells are washed with PBS and RNA is extracted using RNAeasy Plus mini kit.
動物実験 動物モデル 6-8 weeks old FVB mice, prostate PDX model (TM00298), NSG mice, C57BL/6, CB17/Icr-Prkdcscid/IcrIcoCrl mice, CD-1
投薬量 50 mg/kg, 100 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：

A program of successive gene expression in mouse one-cell embryos [ Cell Rep, 2023, 42(2):112023] PubMed: 36729835
Patient-Derived Triple-Negative Breast Cancer Organoids Provide Robust Model Systems That Recapitulate Tumor Intrinsic Characteristics [ Cancer Res, 2022, 82(7):1174-1192] PubMed: 35180770
Loss of G0/G1 switch gene 2 (G0S2) promotes disease progression and drug resistance in chronic myeloid leukaemia (CML) by disrupting glycerophospholipid metabolism [ Clin Transl Med, 2022, 12(12):e1146] PubMed: 36536477
MEK/ERK-mediated oncogenic signals promote secretion of extracellular vesicles by controlling lysosome function [ Cancer Sci, 2022, 113(4):1264-1276] PubMed: 35108425
Yap-Myc signaling induces pancreatic stellate cell activation through regulating glutaminolysis [ Exp Cell Res, 2022, 411(1):113000] PubMed: 34958764
Patient-derived triple negative breast cancer organoids provide robust model systems that recapitulate tumor intrinsic characteristics [ bioRxiv, 2021, 10.1101/2021.08.09.455691] PubMed: None

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。