化合物UNC2250 T1968

Product Introduction
Bioactivity


英文名: UNC2250

描述: UNC2250 是选择性的Mer 抑制剂，其IC50=1.7 nM，分别比相关的激酶 Axl 和 Tyro3 选择性高 160 倍和 60 倍。

细胞实验: BT-12 rhabdoid tumor cells (10?000 cells) are cultured in 2.0 mL of 0.35% soft agar containing 0.5× RPMI medium, 7.5% FBS, and the indicated concentrations of 10 or DMSO vehicle only and overlaid with 0.5 mL of 1× RPMI medium containing 15% FBS and 10 or DMSO vehicle only. Medium and 10 or vehicle are refreshed 2 times per week. Colonies were stained with thiazolyl blue tetrazolium bromide and counted after 3 weeks. Colo699 NSCLC cells (15?000 cells) are cultured in 1.5 mL of 0.35% soft agar containing 1× RPMI medium and 10% FBS and overlaid with 2.0 mL of 1× RPMI medium containing 10% FBS and the indicated concentrations of 10 or DMSO vehicle only. Medium and 10 or vehicle are refreshed 3 times per week. Colonies are stained with nitrotetrazolium blue chloride and counted after 2 weeks.(Only for Reference)

激酶实验: Microfluidic Capillary Electrophoresis (MCE) Assay: Activity assays are performed in a 384-well, polypropylene microplate in a final volume of 50 μL of 50 mM Hepes, pH 7.4, containing 10 mM MgCl2, 1.0 mM DTT, 0.01% Triton X-100, 0.1% bovine serum albumin (BSA), containing 1.0 μM fluorescent substrate and ATP at the Km for each enzyme. All reactions are terminated by addition of 20 μL of 70 mM EDTA. After an 180 min incubation, phosphorylated and unphosphorylated substrate peptides are separated in buffer supplemented with 1× CR-8 on a LabChip EZ Reader equipped with a 12-sipper chip. Data are analyzed using EZ Reader software.

体内活性: 根据体内PK实验，UNC2250具有中等的半衰期、清除率和分布体积，同时具备合理的口服生物利用度和良好的溶解性。[1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 1mg/ml


关键字: UNC 2250 | Tyro3 | Axl | TAM Receptor | inhibit | Mer | Inhibitor | UNC-2250 | UNC2250

相关产品: Bemcentinib | UNC569 | NCT-503 | G-749 | AXL-IN-13 | Gilteritinib hemifumarate | Axl-IN-16 | SGI-7079 | RU-302 | Emactuzumab

相关库: Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途