JHU395

化学情報

溶剤液（一定の濃度）を調合する

生物活性

プロトコル(参考用のみ)

参考

製品コードS8892 バッチS889201

印刷

Synonyms

N/A

Storage
(From the date of receipt)

2 years -20°C liquid

化学式

C₂₂H₂₉N₃O₇

分子量

447.48

CAS No.

2079938-92-2

Solubility (25°C)*

体外

DMSO

100 mg/mL (223.47 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。	5.000mg/ml (11.17mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 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。	2.500mg/ml (5.59mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 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.

細胞アッセイ	細胞株	sNF96.2, sNF02.2, ipn02.32
	濃度	10 μM, 20μM
	反応時間	1 h, 24 h
	実験の流れ	Dose response curves for JHU395 is measured in a 96 well plate by alamar blue fluorescence at 590 nm. 1500-2000 cells per well are plated in standard media or media containing added purine nucleotides (guanosine monophosphate,100μM). One day later media is exchanged for this compound-free media; fixed concentrations of this chemical are added across the plate and cells are incubated for 72 hours prior to dye addition.
動物実験	動物モデル	C57BL6/NHsd (B6) or CD-1 male mice, NPcis (B6;129S2-Trp53^tm1Tyj Nf1^tm1Tyj/J) transgenic mice
	投薬量	1.2 mg/kg, 0.5 mg/kg
	投与方法	Oral gavage

JHU395 is a novel orally bioavailable GA (glutamine antagonists) prodrug designed to circulate inert in plasma, but permeate and release active GA within target tissues. JHU395 delivers active GA to malignant peripheral nerve sheath tumor (MPNST), and significantly inhibits tumor growth without observed toxicity.

in vitro

JHU395 inhibits growth of multiple biosynthetic processes by tumors (MPNST) cells, while growth of immortalized Schwann cells is minimally affected. This compound induces less PARP cleavage as a marker of apoptosis in human MPNST cells. It is a plasma stable lipophilic GA prodrug which delivers DON to MPNST in an in vitro plasma to tumor cell partitioning assay measurement.^[1]

In vivo, orally administered JHU395 delivers active GA to tumors with over twofold higher tumor-to-plasma exposure, and this compound significantly inhibits tumor growth in a murine flank MPNST model without observed toxicity.^[1]

https://pubmed.ncbi.nlm.nih.gov/31594823/

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。