DS18561882

製品コードE1154 バッチE115401

化学情報

	Synonyms		Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₈H₃₁F₃N₄O₆S
	分子量	608.63	CAS No.	2227149-22-4
Solubility (25°C)*	体外	DMSO	100 mg/mL (164.3 mM)
		Ethanol	100 mg/mL (164.3 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	DS18561882 is a potent, tricyclic coumarin-based inhibitor of MTHFD2 with an IC50 of 0.0063 μM, exhibiting significant selectivity over the cytosolic isozyme MTHFD1. It also effectively inhibits tumor growth in mouse xenograft models in vivo.
in vivo	DS18561882 (oral administration; 30, 100 or 300 mg/kg; twice daily) inhibits tumor growth inhibition with a dose-dependent manner, the tumor is completely inhibited (TGI: 67%) at the dose of 300 mg/kg in mice. This compound (oral administration; 10, 30, 100, or 300 mg/kg) has a good oral pharmacokinetic profile, including ACU (64.6, 264, 726 μg.h/ml ); Cmax (11.4, 56.5, 90.1 μg/ml); t1/2 (2.21, 2.16, 2.32 hours) for 30 mg/kg; 100mg/kg; 200 mg/kg, respectively. It is suspended in a 0.5% (w/v) methyl cellulose 400 solution in this article.

製品説明

DS18561882 is a potent, tricyclic coumarin-based inhibitor of MTHFD2 with an IC50 of 0.0063 μM, exhibiting significant selectivity over the cytosolic isozyme MTHFD1. It also effectively inhibits tumor growth in mouse xenograft models in vivo.

in vivo

DS18561882 (oral administration; 30, 100 or 300 mg/kg; twice daily) inhibits tumor growth inhibition with a dose-dependent manner, the tumor is completely inhibited (TGI: 67%) at the dose of 300 mg/kg in mice. This compound (oral administration; 10, 30, 100, or 300 mg/kg) has a good oral pharmacokinetic profile, including ACU (64.6, 264, 726 μg.h/ml ); Cmax (11.4, 56.5, 90.1 μg/ml); t1/2 (2.21, 2.16, 2.32 hours) for 30 mg/kg; 100mg/kg; 200 mg/kg, respectively. It is suspended in a 0.5% (w/v) methyl cellulose 400 solution in this article.

プロトコル(参考用のみ)

参考

https://pubmed.ncbi.nlm.nih.gov/31638799/

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。