MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

NVP-CGM097 sulfate

CAS No. : 1313367-56-4

MCE 国际站：NVP-CGM097 sulfate

产品活性：NVP-CGM097是有效，选择性的MDM2抑制剂；IC₅₀值为1.7 nM。

研究领域：Apoptosis  |  Metabolic Enzyme/Protease

作用靶点：MDM-2/p53  |  E1/E2/E3 Enzyme

In Vitro: NVP-CGM097 binds to human MDM2 with an IC₅₀ of 1.7 nM and shows high selectivity over MDM4 (IC₅₀=2000 nM). NVP-CGM097 is about four times more potent than Nutlin-3a (IC₅₀=8 nM). In addition, NVP-CGM097 shows no significant activity against Bcl-2:Bak, Bcl-2:Bad, Mcl-1:Bak, Mcl-1:NOXA, XIAP:BIR3, and c-IAP:BIR3 protein-protein interactions. NVP-CGM097 significantly inhibits the proliferation of cells expressing wild-type p53, while sparing the p53 null cells with a 35-58-fold difference. NVP-CGM097 is able to significantly redistribute wild-type p53 into the cell nucleus with an IC₅₀ of 0.224 μM, demonstrating its ability to inhibit the p53:MDM2 interaction in living cells. NVP-CGM097 significantly inhibits the proliferation of cells expressing wild-type p53, while sparing the p53 null cells with a 35-58-fold difference. NVP-CGM097 inhibtis HCT116 (p53^WT/WT) with IC₅₀ of 454±136 nM.

In Vivo: NVP-CGM097 is able to inhibit the interaction between p53 and MDM2 and reactivate the p53 pathway in a MDM2-amplified SJSA-1 human tumor model, as judged by elevation of p21 mRNA levels, a pharmacodynamic (PD) indicator for p53 activity. p21 mRNA levels are found to increase concomitantly with levels of NVP-CGM097 in tumor-bearing rats dosed at 30 mg/kg. The PD response is biphasic and prolonged up to 24 h. Additional p53 target genes such as MDM2 and PUMA mRNA levels are assessed in the tumor samples as well and showed a similar behavior. Daily treatment with NVP-CGM097 dose dependently and significantly inhibits SJSA-1 tumor growth in rats. It promotes stable disease at 20 mg/kg, which is associated with a plasma AUC_0-24 of 163 μM•h. After iv administration, the total blood clearance (CL) of NVP-CGM097 is 5 mL/min per kg for mouse, 7 mL/min per kg for rat, 3 mL/min per kg for dog, and 4 mL/min per kg for monkey. The apparent terminal half-life (t_1/2) is long in rodents and monkey (6-12 h) but is comparatively longer in dogs (20 h). After oral dosing, NVP-CGM097 is well absorbed with T_max occurring between 1 and 4.5 h in all species tested.

相关产品：Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Metabolism/Protease Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Oxygen Sensing Compound Library  |  Ubiquitination Compound Library  |  Ferroptosis Compound Library  |  Pyroptosis Compound Library  |  Glutamine Metabolism Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Anti-Cancer Metabolism Compound Library  |  Transcription Factor-Targeted Library  |  Targeted Diversity Library  |  Anti-Liver Cancer Compound Library   |  Anti-Colorectal Cancer Compound Library   |  Protein-protein Interaction Inhibitor Library  |  Highly Selective Inhibitors Library  |  WSB1 Degrader 1  |  GS143  |  p53 (17-26)  |  p53 and MDM2 proteins-interaction-inhibitor (racemic)  |  Navtemadlin  |  Antitumor agent-60  |  Roslin 2 bromide  |  Amifostine trihydrate  |  MX69  |  ADH-6 TFA  |  RG7112  |  SCH529074  |  CBL0137 hydrochloride  |  MA242  |  MD-224  |  MB710  |  WS-383 free base  |  NSC59984  |  MDM2/4-p53-IN-1  |  Oxychlororaphine  |  Ubiquitination-IN-1  |  Pifithrin-β hydrobromide  |  UbcH5c-IN-1  |  p53-MDM2-IN-1  |  PK11000  |  Tenovin-6  |  NSC 146109 hydrochloride  |  Ivaltinostat  |  FOXO4-DRI acetate  |  3-Morpholinosydnonimine

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

货号: HY-15954B

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
•   50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。