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NVP-CGM097

NVP-CGM097

产品编号 TQ0231   CAS 1313363-54-0
别名: CGM097

NVP-CGM097 (CGM097) 是一种选择性MDM2抑制剂,对hMDM2的IC50为 1.7 nM。

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NVP-CGM097 Chemical Structure
NVP-CGM097, CAS 1313363-54-0
规格 价格/CNY 货期 数量
1 mg ¥ 575 现货
2 mg ¥ 837 现货
5 mg ¥ 1,550 现货
10 mg ¥ 2,680 现货
25 mg ¥ 4,490 现货
50 mg ¥ 6,380 现货
100 mg ¥ 8,750 现货
1 mL * 10 mM (in DMSO) ¥ 2,520 现货
其他形式的 NVP-CGM097:
产品目录号及名称: NVP-CGM097 (TQ0231)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 NVP-CGM097 (CGM097) is an effective and specific MDM2 inhibitor (IC50: 1.7 nM for hMDM2).
靶点活性 MDM2:1.7 nM
体外活性 NVP-CGM097 binds to human MDM2(IC50: 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). 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. 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 inhibits HCT116 (p53WT/WT, IC50: 454±136 nM).
体内活性 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 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 AUC0-24 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 (t1/2) 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 Tmax occurring between 1 and 4.5 h in all species tested.
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.
别名 CGM097
分子量 659.26
分子式 C38H47ClN4O4
CAS No. 1313363-54-0

存储

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

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5169 mL 7.5843 mL 15.1685 mL 37.9213 mL
5 mM 0.3034 mL 1.5169 mL 3.0337 mL 7.5843 mL
10 mM 0.1517 mL 0.7584 mL 1.5169 mL 3.7921 mL
20 mM 0.0758 mL 0.3792 mL 0.7584 mL 1.8961 mL
50 mM 0.0303 mL 0.1517 mL 0.3034 mL 0.7584 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Holzer P, et al. Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. J Med Chem. 2015 Aug 27;58(16):6348-58
Cbl-b-IN-6 NAcM-OPT Cbl-b-IN-7 M435-1279 MD-224 Mezigdomide DKM 2-93 PYR-41

相关化合物库

该产品包含在如下化合物库中:
高选择性抑制剂库 抗癌活性化合物库 抗癌临床化合物库 抗癌药物库 HIF-1化合物库 抗癌细胞代谢库 细胞焦亡化合物库 内质网应激化合物库 细胞凋亡化合物库 临床期小分子药物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

NVP-CGM097 1313363-54-0 Apoptosis Ubiquitination E1/E2/E3 Enzyme Mdm2 Ubiquitin ligase inhibit MDM-2/p53 CGM-097 E3 ligating enzyme CGM 097 Ubiquitin activating enzyme NVP CGM097 Inhibitor CGM097 E2 conjugating enzyme NVPCGM097 E1 activating enzyme NVP-CGM-097 Ubiquitin conjugating enzyme NVP-CGM 097 inhibitor

 

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