LYN-1604

製品コードS8597 バッチS859701

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₃₃H₄₅Cl₄N₃O₂

分子量

657.54

CAS No.

2088939-99-3

Solubility (25°C)*

体外

Water

100 mg/mL (152.08 mM)

Ethanol

100 mg/mL (152.08 mM)

DMSO

50 mg/mL (76.04 mM)

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。	4.700mg/ml (7.15mM)	Taking the 1 mL working solution as an example, add 50 μL of 94 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。	0.780mg/ml (1.19mM)	Taking the 1 mL working solution as an example, add 50 μL of 15.6 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	LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants.
in vitro	LYN-1604 is a ULK1 agonist. Three amino acid residues (LYS50, LEU53, and TYR89) are key to the activation site of this compound and ULK1 by site-directed mutagenesis and biochemical assays. It induces cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis. This compound is bound to wild-type ULK1 with a binding affinity in the nanomole range (KD = 291.4 nM), but the ULK1Y89A mutant protein causes a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1K50A and ULK1L53A mutants^[1].
in vivo	LYN-1604 could significantly inhibit the growth of xenograft MDA-MB-231 cells. This compound can directly activate ULK1, the initiator of autophagy, thereby inducing cell death to inhibit the growth of triple negative breast cancer (TNBC) in vitro and in vivo^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MDA-MB-231 cells
	濃度	0.5, 1.0 and 2.0 μM
	反応時間	24 h
	実験の流れ	Cells are dispensed in 96-well plates at a density of 5 × 10⁴ cells per mL. After 24 h of incubation, cells are treated with different concentrations of this compound for the indicated time periods. Cell viability is measured by the MTT assay.
動物実験	動物モデル	MDA-MB-231 xenograft model (BALB/c nude mice)
	投薬量	25 mg/kg, 50 mg/kg, 100 mg/kg
	投与方法	intragastric administration

参考

https://pubmed.ncbi.nlm.nih.gov/28553505/

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：

Piceatannol enhances Beclin-1 activity to suppress tumor progression and its combination therapy strategy with everolimus in gastric cancer [ Sci China Life Sci, 2022, 10.1007/s11427-022-2185-9]	PubMed: 36271983
Synergetic contributions of viral VP1, VP3, and 3C to activation of the AKT-AMPK-MAPK-MTOR signaling pathway for Seneca Valley virus-induced autophagy [ J Virol, 2021, JVI0155021]	PubMed: 34757844
Corneal autophagy and ocular surface inflammation: A new perspective in dry eye. [ Exp Eye Res, 2019, 184:126-134]	PubMed: 31018117

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。