化合物 SCH772984|T6066

17篇文献

SCH772984
942183-80-4

询价 1removed 起订

上海更新日期：2026-08-03

TargetMol中国（陶术生物）

VIP14年

高新技术企业

企业技术中心

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 SCH772984

英文名称：: SCH772984

CAS号：: 942183-80-4

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

纯度规格：: 97.57%

产品类别：: 抑制剂

货号：: T001|T6066

Product Introduction

Bioactivity

名称	SCH772984
描述	SCH772984 is an ERK inhibitor that inhibits ERK1 and ERK2 (IC₅₀=4/1 nM) and is highly selective and ATP-competitive. SCH772984 exhibits antitumor activity against BRAF or RAS mutant cells.
细胞实验	For resistant cell line creation, cells were grown in Dulbecco's modified Eagle medium with 10% heat-inactivated FBS media and increasing concentrations of inhibitor (PLX4032, 0.1–10 μmol/L; GSK1120212, 0.01–1 μmol/L) over approximately 4 to 8 months until resistant cells acquired growth properties similar to na?ve parental cells (at their top drug concentrations). For combination resistance, cells were incubated as above but with alternative dose escalation until a top concentration was acquired (PLX4032 10 μmol/L and GSK1120212 1 μmol/L). Stocks and dilutions of PLX4032, GSK1120212, and SCH772984 were made in DMSO solvent. Cell proliferation experiments were carried out in a 96-well format (six replicates), and cells were plated at a density of 4,000 cells per well. At 24 hours after cell seeding, cells were treated with DMSO or a 9-point IC50 dilution (0.001–10 μmol/L) at a final concentration of 1% DMSO for all concentrations. Viability was assayed 5 days after dosing using the ViaLight luminescence kit following the manufacturer's recommendations (n = 6, mean ± SE). For the cell line panel viability assay, cells were treated with SCH772984 for 4 days and assayed by the CellTiterGlo luminescent cell viability assay. For IncuCyte analysis, cells were plated as above in 96-well plates, and image-based cell confluence data were collected every 2 hours during live growth. For engineered resistant lines, cells were infected with lentivirus produced from lentiORF constructs expressing either RFP, KRASG13D, BRAFV600E, truncated BRAFV600E lacking exons 2–8 (Δ2-8), MEK1P124L, MEK1F129L, or constitutively active MEK1DD (S218D+S222D). Cells were selected in blasticidin (20 μg/mL) and used for ViaLight assays as described above [1].
激酶实验	SCH772984 was tested in 8-point dilution curves in duplicate against purified ERK1 or ERK2. The enzyme was added to the reaction plate and incubated with the compound before adding a solution of substrate peptide and ATP. Fourteen microliters of diluted enzyme (0.3 ng active ERK2 per reaction) was added to each well of a 384-well plate. The plates were gently shaken to mix the reagents and incubated for 45 minutes at room temperature. The reaction was stopped with 60 μL of IMAP Binding Solution (1:2,200 dilutions of IMAP beads in 1× binding buffer). The plates were incubated at room temperature for an additional 0.5 hours to allow complete binding of phosphopeptides to the IMAP beads. Plates were read on the LJL Analyst [1].
动物实验	Nude mice were injected subcutaneously with specific cell lines, grown to approximately 100 mm^3, randomized to treatment groups (10 mice/group), and treated intraperitoneally with either SCH772984 or vehicle according to the dosing schedule indicated in the figure legends. Tumor length (L), width (W), and height (H) were measured during and after the treatment periods by a caliper twice weekly on each mouse and then used to calculate tumor volume using the formula (L × W × H)/2. Animal body weights were measured on the same days twice weekly. Data were expressed as mean ± SEM. Upon completion of the experiment, vehicle- and SCH772984-treated tumor biopsies were processed for Western blot analysis [1].
体外活性	方法: 21 种含有BRAF基因突变的黑色素瘤细胞系用 SCH772984 (0-10 µM) 处理 72-120 h，使用 CellTiter-Glo Luminescent Cell Viability Assay 检测细胞活力。结果: 在 21 种细胞系中，对 SCH-772984 的敏感性分为3组：高敏感性 (IC50< 1 µM)、中敏感性 (IC50= 1-2 µM) 和耐药性 (IC50> 2 µM)。[1] 方法: BRAF 突变体 A375 细胞用 SCH772984 (0.1-2 µmol/L) 处理 4 h，使用 Western Blot 检测靶点蛋白表达水平。结果: Epirubicin 在 G2/M 阻滞中显著增加了 sub-G 细胞。[2]
体内活性	方法: 为检测体内抗肿瘤活性，将 SCH772984 (25-50 mg/kg) 腹腔注射给携带 MiaPaCa 异种移植物的 Nude 小鼠，每天两次，持续十四天。结果: 在两种剂量下均观察到肿瘤消退，25 mg/kg 剂量下肿瘤消退 9%，50 mg/kg 剂量下肿瘤消退 36%。[2]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
溶解度	H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+90% Saline : 0.54 mg/mL (0.92 mM), Solution. DMSO : 16.7 mg/mL (28.42 mM), Sonication is recommended.
关键字	SCH-772984 \| SCH772984 \| SCH 772984 \| Inhibitor \| inhibit \| Extracellular signal regulated kinases \| ERK2 \| ERK1 \| ERK
相关产品	Urea \| Lidocaine hydrochloride \| Lactose \| Nisin Z \| Tauroursodeoxycholate \| Gum arabic \| Gluconate Calcium \| Gluconate sodium \| β-Glycerophosphate disodium salt pentahydrate \| TBHQ \| Trametinib \| L-Cysteine
相关库	抑制剂库 \| 经典已知活性库 \| 抗癌活性化合物库 \| 已知活性化合物库 \| 激酶抑制剂库 \| 抗纤维化化合物库 \| 细胞凋亡化合物库 \| 抗衰老化合物库 \| 高选择性抑制剂库 \| HIF-1化合物库 \| 免疫/炎症分子化合物库 \| 疼痛相关化合物库

SCH772984;TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(14年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子