优立替尼
基本信息
产品名称：
优立替尼
英文名称：
Ulixertinib
国产/进口：
进口
产地/品牌：
美国/TargetMol
型号：
参考报价：
面议
销售商：
总点击数：
64
更新日期：
2025-08-11
产品类别：
性能参数
Product Introduction
Bioactivity
英文名: Ulixertinib
描述: Ulixertinib (VRT752271) 是一种有效且可逆的 ERK1/ERK2 抑制剂，可抑制 ERK2 和下游蛋白 RSK 的磷酸化，对 ERK2 的IC50值小于 0.3 nM。
细胞实验: A375 cells are cultured in cell media composed of DMEM, 10% (v/v) Foetal Calf Serum and 1% (v/v) L-Glutamine. After harvesting, cells are dispensed into black, 384-well Costar plates to give 200 cells per well in a total volume of 40 μL cell media, and are incubated overnight at 37°C, 90% relative humidity and 5% CO2 in a rotating incubator. Test compounds and reference controls are dosed directly into the cell plates, into the inner 308 wells, using a Labcyte Echo 555 acoustic dispenser. The cells are dosed over a 12 point range from 30 μM down to 0.03 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 0.3%. The cell plates are then incubated for 72 hours at 37°C. Cells were fixed and stained by the addition of 20 μL 12% formaldehyde in PBS/A (4% final concentration) and 1:2000 dilution of Hoechst 33342, with a 30 minute room temperature incubation, and then washed with PBS/A. A cell count is performed on the stained cell plates using a Cellomics ArrayScanTM VTI imaging platform. A Day 0 cell plate is also fixed, stained and read to generate a cell count baseline for determining compound cytotoxic effects as well as anti-proliferative effects.(Only for Reference)
激酶实验: ERK2 Rapidfire Mass Spectrometry Inhibition of Catalysis Assay: MEK U911-activated ERK2 protein is expressed and purified in-house. Enzyme and substrate solutions are made up in assay buffer consisting of 50 mM Tris (pH 7.5), 10 mM MgCl2, 0.1 mM EGTA, 10 mM DTT and 0.01% (v/v) CHAPS. 1.2 nM ERK2 protein is prepared in assay buffer and 10 μL is dispensed into each well of a polypropylene, 384-well plate containing test and reference control compounds. The compound plates had previously been dosed with a 12 point range from 100 μM down to 0.1 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 1%. Following a 20 minute pre-incubation of enzyme and compound at room temperature, 10 μL of substrate solution is added consisting of 16 μM Erktide (IPTTPITTTYFFFK) and 120 μM ATP (measured Km) in assay buffer. The reaction is allowed to progress for 20 minutes at room temperature before being quenched by the addition of 80 μl 1% (v/v) formic acid. The assay plates are then run on the RapidFire Mass Spectrometry platform to measure substrate (unphosphorylated Erktide) and product (phosphorylated Erktide) levels.
体外活性: 在含有b-RAFV600E突变的A375黑色素瘤细胞株中，Ulixertinib分别以IC50为4.1/0.14 μM降低磷酸化ERK2（pERK）和下游激酶RSK（pRSK）的水平。同时，Ulixertinib以IC50为180 nM抑制A375细胞的增殖。[1]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 80 mg/mL (184.6 mM)
5% DMSO+95% Saline : 4 mg/mL (9.23 mM, suspension)
Ethanol : 12 mg/mL (27.7 mM)
关键字: ERK | VRT 752271 | inhibit | BVD 523 | Ulixertinib | VRT-752271 | BVD523 | Inhibitor | Extracellular signal regulated kinases
相关产品: ERK5-IN-1 | Corynoxeine | Dehydroeffusol | Lidocaine | Licochalcone D | Tetrahydrocoptisine | Asperulosidic acid | SCH772984 HCl | Lup-20(29)-en-28-oic acid | MK-8353
相关库: Drug Repurposing Compound Library | HIF-1 Signaling Pathway Compound Library | Anti-Cancer Drug Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Apoptosis Compound Library | Autophagy Compound Library | Orally Active Compound Library
Bioactivity
英文名: Ulixertinib
描述: Ulixertinib (VRT752271) 是一种有效且可逆的 ERK1/ERK2 抑制剂，可抑制 ERK2 和下游蛋白 RSK 的磷酸化，对 ERK2 的IC50值小于 0.3 nM。
细胞实验: A375 cells are cultured in cell media composed of DMEM, 10% (v/v) Foetal Calf Serum and 1% (v/v) L-Glutamine. After harvesting, cells are dispensed into black, 384-well Costar plates to give 200 cells per well in a total volume of 40 μL cell media, and are incubated overnight at 37°C, 90% relative humidity and 5% CO2 in a rotating incubator. Test compounds and reference controls are dosed directly into the cell plates, into the inner 308 wells, using a Labcyte Echo 555 acoustic dispenser. The cells are dosed over a 12 point range from 30 μM down to 0.03 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 0.3%. The cell plates are then incubated for 72 hours at 37°C. Cells were fixed and stained by the addition of 20 μL 12% formaldehyde in PBS/A (4% final concentration) and 1:2000 dilution of Hoechst 33342, with a 30 minute room temperature incubation, and then washed with PBS/A. A cell count is performed on the stained cell plates using a Cellomics ArrayScanTM VTI imaging platform. A Day 0 cell plate is also fixed, stained and read to generate a cell count baseline for determining compound cytotoxic effects as well as anti-proliferative effects.(Only for Reference)
激酶实验: ERK2 Rapidfire Mass Spectrometry Inhibition of Catalysis Assay: MEK U911-activated ERK2 protein is expressed and purified in-house. Enzyme and substrate solutions are made up in assay buffer consisting of 50 mM Tris (pH 7.5), 10 mM MgCl2, 0.1 mM EGTA, 10 mM DTT and 0.01% (v/v) CHAPS. 1.2 nM ERK2 protein is prepared in assay buffer and 10 μL is dispensed into each well of a polypropylene, 384-well plate containing test and reference control compounds. The compound plates had previously been dosed with a 12 point range from 100 μM down to 0.1 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 1%. Following a 20 minute pre-incubation of enzyme and compound at room temperature, 10 μL of substrate solution is added consisting of 16 μM Erktide (IPTTPITTTYFFFK) and 120 μM ATP (measured Km) in assay buffer. The reaction is allowed to progress for 20 minutes at room temperature before being quenched by the addition of 80 μl 1% (v/v) formic acid. The assay plates are then run on the RapidFire Mass Spectrometry platform to measure substrate (unphosphorylated Erktide) and product (phosphorylated Erktide) levels.
体外活性: 在含有b-RAFV600E突变的A375黑色素瘤细胞株中，Ulixertinib分别以IC50为4.1/0.14 μM降低磷酸化ERK2（pERK）和下游激酶RSK（pRSK）的水平。同时，Ulixertinib以IC50为180 nM抑制A375细胞的增殖。[1]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 80 mg/mL (184.6 mM)
5% DMSO+95% Saline : 4 mg/mL (9.23 mM, suspension)
Ethanol : 12 mg/mL (27.7 mM)
关键字: ERK | VRT 752271 | inhibit | BVD 523 | Ulixertinib | VRT-752271 | BVD523 | Inhibitor | Extracellular signal regulated kinases
相关产品: ERK5-IN-1 | Corynoxeine | Dehydroeffusol | Lidocaine | Licochalcone D | Tetrahydrocoptisine | Asperulosidic acid | SCH772984 HCl | Lup-20(29)-en-28-oic acid | MK-8353
相关库: Drug Repurposing Compound Library | HIF-1 Signaling Pathway Compound Library | Anti-Cancer Drug Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Apoptosis Compound Library | Autophagy Compound Library | Orally Active Compound Library
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TargetMol（陶术）作为一家全球性的生物医药领域高科技企业，我们致力于为高校、研究所、医院、企业等各类生物医药研发机构提供优质的产品和服务，为全球医药科学家更高效地完成科研工作助力。可提供20,000+种 抑制剂和激动剂 、800+种 化合物库 、19,000+种 天然产物 ，以及9,000+种 重组蛋白 、多种 多肽 、抗体 和 生命科学试剂盒 等。此外，在上海，TargetMol研发中心配备了 CADD & AIDD研究中心、药理实验室和药物化学合成 平台三大技术中心，可提供虚拟筛选、化合物活性测试、分子间结合力检测和化合物结构优化等技术服务，多方位满足用户的研发需求。
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