MYCi361

製品コードS8905 バッチS890501

印刷

化学情報

Synonyms

NUCC-0196361

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₆H₁₆ClF₉N₂O₂

分子量

594.86

CAS No.

2289690-31-7

Solubility (25°C)*

体外

DMSO

100 mg/mL (168.1 mM)

Ethanol

14 mg/mL (23.53 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。	2.500mg/ml (4.20mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 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 make it clear; 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	MYCi361 (NUCC-0196361) is a MYC inhibitor that engages MYC inside cells, disrupts MYC/MAX dimers, and impairs MYC-driven gene expression. MYCi361 binds to MYC with Kd of 3.2 μM. MYCi361 suppresses in vivo tumor growth, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy.
in vitro	MYCi361 engages MYC inside cells, disrupts MYC/MAX dimers, and impairs MYC-driven gene expression. This compound enhances MYC phosphorylation on threonine-58, consequently increasing proteasome-mediated MYC degradation.^[1]
in vivo	MYCi361 suppresses in vivo tumor growth in mice, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy.^[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, TGR-1, HO15.19 Rat-1 cells
	濃度	4 μM
	反応時間	72 h
	実験の流れ	Immunogenic Cell Death Assays: MycCaP cells are treated with 4 μM MYCi361 for 72 hr, and supernatants are collected. Cell counts are performed for quantifying secreted ATP and high mobility group protein B1 (HMGB1). For detection of surface Calreticulin, cells are incubated with rabbit anti-Calreticulin for 60 min and then incubated with Alexa Flour 488 anti-rabbit secondary antibody, and analyzed by flow cytometry.
動物実験	動物モデル	6-8 week old FVB mice, prostate PDX model, NSG mice, C57BL/6 mice, CB17/Icr-Prkdcscid/IcrIcoCrl mice, CD-1 mice
	投薬量	55 mg/kg, 50 mg/kg
	投与方法	IP, Oral gavage

参考

https://pubmed.ncbi.nlm.nih.gov/31679823/

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 Potential Role for c-MYC in the Regulation of Meibocyte Cell Stress [ Cells, 2025, 14(10)709]	PubMed: 40422212
Cell-based high-throughput screening using a target-NanoLuc fusion construct to identify molecular glue degraders of c-Myc oncoprotein [ RSC Chem Biol, 2025, 10.1039/d5cb00093a]	PubMed: 40978459
Genome-scale clustered regularly interspaced short palindromic repeats screen identifies nucleotide metabolism as an actionable therapeutic vulnerability in diffuse large B-cell lymphoma [ Haematologica, 2024, 109(12):3989-4006]	PubMed: 38841800
Extrachromosomal circular DNA promotes prostate cancer progression through the FAM84B/CDKN1B/MYC/WWP1 axis [ Cell Mol Biol Lett, 2024, 29(1):103]	PubMed: 38997648
Inhibiting BRAF/EGFR/MEK suppresses cancer stemness and drug resistance of primary colorectal cancer cells [ Oncotarget, 2023, 14:879-889]	PubMed: 37791907
Inhibiting BRAF/EGFR/MEK suppresses cancer stemness and drug resistance of primary colorectal cancer cells [ Oncotarget, 2023, 10.18632/oncotarget.28517]	PubMed: 37791907
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
Circular RNA circ_0057558 Controls Prostate Cancer Cell Proliferation Through Regulating miR-206/USP33/c-Myc Axis [ Front Cell Dev Biol, 2021, 9:644397]	PubMed: 33718387

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。