SAR405

製品コードS7682 バッチS768201

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	C₁₉H₂₁ClF₃N₅O₂
	分子量	443.85	CAS No.	1523406-39-4
Solubility (25°C)*	体外	DMSO	88 mg/mL (198.26 mM)
		Ethanol	88 mg/mL (198.26 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	SAR405は、高選択性を示し、クラスIおよびクラスIIのPI3KやmTORに対して10 μMまで活性を示さない、低分子量のPIK3C3/Vps34キナーゼ阻害剤（KD 1.5 nM）です。SAR405はオートファジーを抑制し、腫瘍細胞におけるMTOR（rapamycinのメカニズム的標的）阻害と相乗効果を発揮します。
in vitro	SAR405 is an inhibitor that was highly specific for Vps34 with regard to protein kinases and other phosphoinositide kinases. This compound has an IC50 of 1 nM in the phosphorylation of a PtdIns substrate by human recombinant Vps34 enzyme. It shows a binding equilibrium constant KD of 1.52 ± 0.77 nM (± s.d.) and a dissociation rate constant, k_off, of 3.03 ± 0.55 10⁻³/s, corresponding to a residence half-life, t_1/2, of 3.8 min. This inhibitor does not affect the Akt phosphorylation at concentrations up to 10 μM in the PC3 cell line. It affects vesicle trafficking from late endosomes to lysosomes. It is also a potent autophagy inhibitor.
in vivo	SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	GFP-LC3 HeLa cells
	濃度	1 μM
	反応時間	4 h
	実験の流れ	GFP-LC3 HeLa cells are starved for 2 h in EBSS plus 10 μM this compound or DMSO. For mTOR inhibitor, GFP-LC3 H1299 cells are treated with 1 μM AZD8055 for 4 h in fed conditions. Cells are then fixed with 4% PFA, and nuclei are stained using 2 μg/ml Hoechst 33342. Fluorescence is analyzed using an imaging cytometer. Cells are considered positive when there are more than four green spots per cell, with a total of 25 fields acquired. The activity of the product is estimated.
動物実験	動物モデル	Nude mice
	投薬量	2 mg/kg
	投与方法	s.c.

参考

https://pubmed.ncbi.nlm.nih.gov/25326666/
https://pubmed.ncbi.nlm.nih.gov/33235386/

カスタマーフィードバック

: Data from [Data independently produced by , , Urol Oncol, 2018, 36(4):160.e1-160.e13]

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：

Oncogenic RAS induces a distinctive form of non-canonical autophagy mediated by the P38-ULK1-PI4KB axis [ Cell Res, 2025, 10.1038/s41422-025-01085-9]	PubMed: 40055523
A chaperone-proteasome-based fragmentation machinery is essential for aggrephagy [ Nat Cell Biol, 2025, 27(9):1448-1464]	PubMed: 40866512
Kit-mediated autophagy suppression driven by a viral oncoprotein emerges as a crucial survival mechanism in Merkel cell carcinoma [ Autophagy, 2025, 21(7):1523-1543]	PubMed: 40108758
Host PIK3C3 promotes Shigella flexneri spread from cell to cell through vacuole formation [ PLoS Pathog, 2025, 21(5):e1012707]	PubMed: 40378153
Multiple interactions mediate the localization of BLTP2 at ER-PM contacts to control plasma membrane dynamics [ bioRxiv, 2025, 2025.02.07.637094]	PubMed: 39974967
STING orchestrates the neuronal inflammatory stress response in multiple sclerosis [ Cell, 2024, 187(15):4043-4060.e30]	PubMed: 38878778
Intercellular transfer of cancer cell invasiveness via endosome-mediated protease shedding [ Nat Commun, 2024, 15(1):1277]	PubMed: 38341434
Targeting autophagy overcomes cancer-intrinsic resistance to CAR-T immunotherapy in B-cell malignancies [ Cancer Commun (Lond), 2024, 44(3):408-432]	PubMed: 38407943
Shigella generates distinct IAM subpopulations during epithelial cell invasion to promote efficient intracellular niche formation [ Eur J Cell Biol, 2024, 103(1):151381]	PubMed: 38183814
Combining VPS34 inhibitors with STING agonists enhances type I interferon signaling and anti-tumor efficacy [ Mol Oncol, 2024, 10.1002/1878-0261.13619]	PubMed: 38506049

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。