UNC2025

製品コードS9662 バッチS966201

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₈H₄₀N₆O
	分子量	476.66	CAS No.	1429881-91-3
Solubility (25°C)*	体外	DMSO	100 mg/mL (209.79 mM)
		Ethanol	60 mg/mL (125.87 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	UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM, 8.18 nM and 364 nM, respectively.
in vitro	Kinome profiling versus more than 300 kinases in vitro and cellular selectivity assessments demonstrate that UNC2025 has similar subnanomolar activity against Flt3, an additional important target in acute myelogenous leukemia (AML), with pharmacologically useful selectivity versus other kinases examined.^[1]
in vivo	UNC2025 is a potent and highly orally bioavailable Mer inhibitor that is capable of inhibiting Mer phosphorylation in vivo, following oral dosing as demonstrated by pharmaco-dynamic (PD) studies examining phospho-Mer in leukemic blasts from mouse bone marrow.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	697 B-ALL, A549 NSCLC, Molm-14 AML cell lines
	濃度	2 nM, 4 nM, 8 nM, 10 nM, 12 nM, 16 nM, 20 nM, 30 nM, 40 nM, 50 nM
	反応時間	1 h
	実験の流れ	697 Cells are treated with the indicated concentrations of UNC2025 for 1 h. Pervanadate is added to cultures for 3 min to stabilize the phosphorylated form of Mer. Mer is immunoprecipitated from cell lysates, and total MER protein and Mer phosphoprotein (p-Mer) are detected by immunoblot.
動物実験	動物モデル	NOD/SCID/gamma mice
	投薬量	3 mg/kg
	投与方法	Oral gavage

参考

[1] Weihe Zhang, et al. J Med Chem. 2014 Aug 28;57(16):7031-41.

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：

Regulation of brain endothelial cell physiology by the TAM receptor tyrosine kinase Mer [ Commun Biol, 2023, 6(1):916]	PubMed: 37673933
Regulation of brain endothelial cell physiology by the TAM receptor tyrosine kinase Mer [ Commun Biol, 2023, 6(1):916]	PubMed: 37673933
The Tolerogenic Influence of Dexamethasone on Dendritic Cells Is Accompanied by the Induction of Efferocytosis, Promoted by MERTK [ Int J Mol Sci, 2023, 10.3390/ijms242115903]	PubMed: 37958886
Intranasal delivery of a small-molecule ErbB inhibitor promotes recovery from acute and late-stage CNS inflammation [ JCI Insight, 2022, 7(7)e154824]	PubMed: 35393953
Expression of TAM-R in Human Immune Cells and Unique Regulatory Function of MerTK in IL-10 Production by Tolerogenic DC [ Front Immunol, 2020, 11:564133]	PubMed: 33101282
New insights into Notch1 regulation of the PI3K-AKT-mTOR1 signaling axis: targeted therapy of γ-secretase inhibitor resistant T-cell acute lymphoblastic leukemia [ Cell Signal, 2014, 26(1):149-61]	PubMed: 24140475

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。