化合物NVP-CGM097 TQ0231
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
2 mg | 1313363-54-0 | ¥695.00 | 询底价 |
1 mL | 1313363-54-0 | ¥1,920.00 | 询底价 |
5 mg | 1313363-54-0 | ¥1,320.00 | 询底价 |
10 mg | 1313363-54-0 | ¥2,230.00 | 询底价 |
1 mg | 1313363-54-0 | ¥477.00 | 询底价 |
100 mg | 1313363-54-0 | ¥7,280.00 | 询底价 |
25 mg | 1313363-54-0 | ¥3,730.00 | 询底价 |
50 mg | 1313363-54-0 | ¥5,290.00 | 询底价 |
Product Introduction
Bioactivity
英文名: NVP-CGM097
描述: NVP-CGM097 (CGM097) 是一种选择性MDM2抑制剂,对hMDM2的IC50为 1.7 nM。
细胞实验: Two pairs of cell lines are used to assess NVP-CGM097 p53-dependent antiproliferative effects: (1) an isogenic pair of HCT116 cell lines either expressing wild-type p53 or knocked-out for the p53 gene and (2) a nonisogenic pair of osteosarcoma cell lines either endogenously expressing wild-type p53 and amplified for MDM2 (SJSA-1 cells) or null for p53 (SAOS-2 cells).
动物实验: Female athymic rats bearing subcutaneous xenotransplants of SJSA-1 tumors (n=5-12) are treated at 5, 10, 20, or 30 mg/kg or three times a week on Monday, Wednesday, and Friday (3qw M, W, F) at 30 or 70 mg/kg p.o for 14 days. Plasma AUCs are determined at the end of the study. Positive numbers indicate the percentage of tumor growth inhibition (T/C); negative numbers indicate the percentage of tumor regression.
体外活性: NVP-CGM097 与人类 MDM2 (IC50: 1.7 nM) 结合,并显示出对 MDM4 (IC50: 2000 nM) 的高选择性。NVP-CGM097 的效力约为 Nutlin-3a (IC50: 8 nM) 的四倍。NVP-CGM097 显著抑制表达野生型 p53 的细胞增殖,而对 p53 空缺细胞影响较小,两者之间的差异为 35-58 倍。NVP-CGM097 能够显著地将野生型 p53 重新分布到细胞核中,其 IC50 为 0.224 μM。此外,NVP-CGM097 对于 HCT116 (p53WT/WT, IC50: 454±136 nM) 也表现出了抑制作用。
体内活性: 在肿瘤携带的大鼠中,随着NVP-CGM097水平的同时增加,发现p21 mRNA水平在30 mg/kg的剂量下上升。PD反应呈双相性并持续至24小时。同样,评估肿瘤样本中的其他p53靶基因(如MDM2和PUMA mRNA水平)也显示出类似行为。每日用NVP-CGM097治疗能剂量依赖性且显著抑制大鼠的SJSA-1肿瘤生长。在20 mg/kg的剂量下促成稳定疾病,与此相关的血浆AUC0-24为163 μM•h。经静脉给药后,NVP-CGM097的总血液清除率(CL)对于小鼠为5 mL/min每kg,大鼠为7 mL/min每kg,狗为3 mL/min每kg,猴子为4 mL/min每kg。表观终末半衰期(t1/2)在啮齿动物和猴子中较长(6-12小时),但在狗中相对更长(20小时)。经口给药后,NVP-CGM097吸收良好,所有测试物种的Tmax在1至4.5小时之间。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 48 mg/mL (72.81 mM )
H2O : Insoluble
关键字: Ubiquitin ligase | inhibit | MDM-2/p53 | CGM-097 | E3 ligating enzyme | CGM 097 | Ubiquitin activating enzyme | NVP CGM097 | Inhibitor | E1/E2/E3 Enzyme | E2 conjugating enzyme | NVPCGM097 | E1 activating enzyme | NVP-CGM-097 | Ubiquitin conjugating enzyme | NVP-CGM097 | NVP-CGM 097
相关产品: IVHD-valtrate | SAR405838 | MMRi64 | MX69 | Kevetrin hydrochloride | Serdemetan | Nutlin-3b | Milademetan | SJ-172550 | Triptolide
相关库: Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Anti-Lung Cancer Compound Library | Ferroptosis Compound Library | Ubiquitination Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Highly Selective Inhibitor 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