GSK3368715 3HCl

製品コードS8858 バッチS885801

印刷

化学情報

Synonyms

EPZ019997 3HCl

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₀H₄₁Cl₃N₄O₂

分子量

475.92

CAS No.

2227587-26-8

Solubility (25°C)*

体外

DMSO

81 mg/mL (170.19 mM)

Water

81 mg/mL (170.19 mM)

Ethanol

81 mg/mL (170.19 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。	4.050mg/ml (8.51mM)	Taking the 1 mL working solution as an example, add 50 μL of 81 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。	0.675mg/ml (1.42mM)	Taking the 1 mL working solution as an example, add 50 μL of 13.5 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	GSK3368715 3HClは、PRMT1、3、4、6、および8を1.5〜81 nMのKi^app値で阻害するI型タンパク質アルギニンメチルトランスフェラーゼ（PRMT）の強力な阻害剤です。
in vitro	GSK3368715 is a potent, reversible, SAM uncompetitive inhibitor of type I PRMTs that produces a shift in arginine methylation states on hundreds of substrates from ADMA to MMA and SDMA. As a monotherapy, GSK3368715 induces anti-proliferative effects on cell lines from a broad range of hematological and solid tumor types in vitro.
in vivo	GSK3368715 has potent, anti-proliferative activity across cell lines representing a range of solid and hematological malignancies and can completely inhibit tumor growth or cause regressions of tumor models in vivo.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	249 cancer cell lines (Toledo cells, BxPC3 cells, MiaPaca-2 cells, ACHN cells, MDA-MB-468 cells, RKO cells, Panc03.27 cells, etc.)
	濃度	0.75 nM, 2 μM
	反応時間	30 min, 3 h - 168 h
	実験の流れ	In Cell Western. RKO cells are seeded in a clear bottom 384 well plates andtreated with a 20-point two-fold dilution series of GSK3368715 (29,325.5 to 0.03 nM) or 0.15% DMSO. Plates are incubated for 3 days at 37℃ in 5% CO₂. Cells are fixed with ice-cold methanol for 30 minutes at room temperature, washed with phosphate buffered saline (PBS), then incubated with Odyssey blocking buffer (Licor) for 1 hour at room temperature.
動物実験	動物モデル	Female NMRI nu/nu mice (NMRI-Foxn1nu) implanted with tumor fragment
	投薬量	75 mg/kg, 150 mg/kg, 300 mg/kg
	投与方法	Oral gavage

参考

https://pubmed.ncbi.nlm.nih.gov/31257072/

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：

PRMT1 mediated methylation of cGAS suppresses anti-tumor immunity [ Nat Commun, 2023, 14(1):2806]	PubMed: 37193698
FACS-based genome-wide CRISPR screens define key regulators of DNA damage signaling pathways [ Mol Cell, 2023, 83(15):2810-2828.e6]	PubMed: 37541219
Epigenetic drug screening defines a PRMT5 inhibitor-sensitive pancreatic cancer subtype [ JCI Insight, 2022, 7(10)e151353]	PubMed: 35439169
Modulation of IKs channel-PIP2 interaction by PRMT1 plays a critical role in the control of cardiac repolarization [ J Cell Physiol, 2022, 10.1002/jcp.30775]	PubMed: 35580065
Purification and Identification of Natural Inhibitors of Protein Arginine Methyltransferases from Plants [ Mol Cell Biol, 2022, e0052321]	PubMed: 35311588

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。