Nutlin3(CAS 548472-68-0)产品图片
Nutlin3CAS号548472-68-0
Nutlin3CAS号548472-68-0
Nutlin3CAS号548472-68-0

Nutlin3

¥340.00 ~¥5,610.00
5mg / 1mg / 10mg / 25mg / 50mg / 100mg
5mg
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索莱宝
2026-05-09
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产品详情与公司简介

产品详情

Nutlin3 基本信息
中文名称:Nutlin3中文别名:Nutlin3
英文名称:Nutlin3CAS:548472-68-0
产品分类:小分子化合物纯度:≥98%
Nutlin3 规格价格信息
产品编号品牌纯度规格库存价格
IN4610索莱宝≥98%5mg有现货870.00 元
IN4610索莱宝≥98%1mg有现货340.00 元
IN4610索莱宝≥98%10mg有现货1,290.00 元
IN4610索莱宝≥98%25mg有现货2,420.00 元
IN4610索莱宝≥98%50mg有现货3,870.00 元
IN4610索莱宝≥98%100mg有现货5,610.00 元
Nutlin3 CAS 属性信息
标准名称:4-[4,5-双(4-氯苯基)-2-(4-甲氧基-2-异丙氧基苯基)-4,5-二氢咪唑-1-羰基]哌嗪-2-酮英文名称:Nutlin-3
CAS:548472-68-0分子式:C30H30Cl2N4O4
分子量:581.489605426788颜色与性状:固体
密度:沸点:
熔点:水溶性:
CAS548472-68-0
英文名称Nutlin3
分子式C30H30Cl2N4O4
分子量581.49
规格5mg ; 1mg ; 10mg ; 25mg ; 50mg ; 100mg
溶解性Soluble in DMSO ≥5mg/mL
纯度≥98%
级别Cell Culture
外观(性状)White to off-white Solid
储存条件Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
运输条件冷藏运输
MDLMFCD07784509
SMILESCC(C)OC1=C(C=CC(=C1)OC)C2=NC(C(N2C(=O)N3CCNC(=O)C3)C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl
InChIKeyBDUHCSBCVGXTJM-UHFFFAOYSA-N
InChIInChI=1S/C30H30Cl2N4O4/c1-18(2)40-25-16-23(39-3)12-13-24(25)29-34-27(19-4-8-21(31)9-5-19)28(20-6-10-22(32)11-7-20)36(29)30(38)35-15-14-33-26(37)17-35/h4-13,16,18,27-28H,14-15,17H2,1-3H3,(H,33,37)
PubChem CID216345
靶点MDM-2
通路Apoptosis
背景说明是一种 MDM2 拮抗剂,抑制 MDM2-p53 相互作用 。
生物活性Nutlin-3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.[1-3]
生物活性Nutlin-3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.[1-3]
IC50Ki: 90 nM (p53-MDM2)[1]
IC50Ki: 90 nM (p53-MDM2)[1]
In VitroNutlin-3 is an inhibitor of the MDM2-p53 interaction. In particular, co-treatment of p53-positive HCT116 cells with 1 μM of Inauhzin and 2 μM of Nutlin-3 more significantly activated p53 as measured by its protein level as well as the level of its target p21, PUMA or cleaved PARP as indication of apoptosis[2]. Nutlin-3 is a small-molecule inhibitor that acts to inhibit MDM2 binding to p53 and subsequent p53-dependent DNA damage signaling. As a single agent, Nutlin-3 (2-10 μM) stabilizes p53 and p21WAF levels and is toxic to WTp53-22RV1 cells (IC50, 4.3 μM) but has minimal toxicity toward p53-deficient cells (IC50, >10 μM). Nutlin-3 induces p53 and p21WAF expression in a dose-dependent manner in 22RV1 cells. Short-term cell cycle assays show that, at a dose of 10 μM, Nutlin-3 increasea slightly the G1-phase fraction and decreasea S-phase fraction of all three cell lines[3].
In VitroNutlin-3 is an inhibitor of the MDM2-p53 interaction. In particular, co-treatment of p53-positive HCT116 cells with 1 μM of Inauhzin and 2 μM of Nutlin-3 more significantly activated p53 as measured by its protein level as well as the level of its target p21, PUMA or cleaved PARP as indication of apoptosis[2]. Nutlin-3 is a small-molecule inhibitor that acts to inhibit MDM2 binding to p53 and subsequent p53-dependent DNA damage signaling. As a single agent, Nutlin-3 (2-10 μM) stabilizes p53 and p21WAF levels and is toxic to WTp53-22RV1 cells (IC50, 4.3 μM) but has minimal toxicity toward p53-deficient cells (IC50, >10 μM). Nutlin-3 induces p53 and p21WAF expression in a dose-dependent manner in 22RV1 cells. Short-term cell cycle assays show that, at a dose of 10 μM, Nutlin-3 increasea slightly the G1-phase fraction and decreasea S-phase fraction of all three cell lines[3].
In VivoNutlin-3 can suppress the growth of xenograft tumors derived from human osteosarcoma or leukemia cells, the anti-tumor activity of Nutlin-3 even at the dose of 200 mg/kg per oral administration is marginal in an HCT116-derived xenograft tumor model[2]. Nutlin-3 may be a useful adjunct to improve the therapeutic ratio using precision radiotherapy targeted to hypoxic cells and warrants further study in vivo[3].
In VivoNutlin-3 can suppress the growth of xenograft tumors derived from human osteosarcoma or leukemia cells, the anti-tumor activity of Nutlin-3 even at the dose of 200 mg/kg per oral administration is marginal in an HCT116-derived xenograft tumor model[2]. Nutlin-3 may be a useful adjunct to improve the therapeutic ratio using precision radiotherapy targeted to hypoxic cells and warrants further study in vivo[3].
细胞实验Human non-small-cell lung carcinoma wild type p53-containing H460 and A549, human non-small-cell lung carcinoma p53-null H1299, and human colon cancer HCT116 (p53+/+ and p53-/-) cells are used. Cells (1.5×105) are plated into 6-well plates, and incubated at 37°C overnight. After treatment of Inauhzin and Nutlin 3 at the indicated concentrations for 48 h, cells are harvested, fixed in 70% ice-cold ethanol overnight at -20°C, resuspended in propidium iodide-solution (50 μg/mL PI, 0.1 mg/mL RNase A, 0.05% Tritin X-100 in PBS) for 40 min at 37°C, then analyzed for DNA content using a flow cytometer and proprietary software[2].
细胞实验Human non-small-cell lung carcinoma wild type p53-containing H460 and A549, human non-small-cell lung carcinoma p53-null H1299, and human colon cancer HCT116 (p53+/+ and p53-/-) cells are used. Cells (1.5×105) are plated into 6-well plates, and incubated at 37°C overnight. After treatment of Inauhzin and Nutlin 3 at the indicated concentrations for 48 h, cells are harvested, fixed in 70% ice-cold ethanol overnight at -20°C, resuspended in propidium iodide-solution (50 μg/mL PI, 0.1 mg/mL RNase A, 0.05% Tritin X-100 in PBS) for 40 min at 37°C, then analyzed for DNA content using a flow cytometer and proprietary software[2].
动物实验Mice[2] Five-week-old female SCID mice are used. Mice are subcutaneously inoculated with 3×106 HCT116p53+/+ cells in the right flank and tumor growth is monitored with calipers. After the mean tumor volume reaches 50-100 mm3, animals are administered Inauhzin intraperitoneally (IP), Nutlin 3 orally, or vehicles (4% DMSO for Inauhzin, EtOH: Tween: 5% Glucose=5:5:90 for Nutlin 3). Tumor volume is measured every other day, and inhibition of tumor growth (T/C) is calculated on the last day of treatment.
动物实验Mice[2] Five-week-old female SCID mice are used. Mice are subcutaneously inoculated with 3×106 HCT116p53+/+ cells in the right flank and tumor growth is monitored with calipers. After the mean tumor volume reaches 50-100 mm3, animals are administered Inauhzin intraperitoneally (IP), Nutlin 3 orally, or vehicles (4% DMSO for Inauhzin, EtOH: Tween: 5% Glucose=5:5:90 for Nutlin 3). Tumor volume is measured every other day, and inhibition of tumor growth (T/C) is calculated on the last day of treatment.
数据来源文献[1]. Yu Z, et al. Design, synthesis and biological evaluation of sulfamide and triazole benzodiazepines as novel p53-MDM2 inhibitors. Int J Mol Sci. 2014 Sep 5;15(9):15741-53.
[2]. Zhang Y, et al. Inauhzin and Nutlin3 synergistically activate p53 and suppress tumor growth.Cancer Biol Ther. Cancer Biol Ther. 2012 Aug;13(10):915-24.
[3]. Supiot S, et al. Nutlin-3 radiosensitizes hypoxic prostate cancer cells independent of p53. Mol Cancer Ther. 2008 Apr;7(4):993-9.
数据来源文献[1]. Yu Z, et al. Design, synthesis and biological evaluation of sulfamide and triazole benzodiazepines as novel p53-MDM2 inhibitors. Int J Mol Sci. 2014 Sep 5;15(9):15741-53.
[2]. Zhang Y, et al. Inauhzin and Nutlin3 synergistically activate p53 and suppress tumor growth.Cancer Biol Ther. Cancer Biol Ther. 2012 Aug;13(10):915-24.
[3]. Supiot S, et al. Nutlin-3 radiosensitizes hypoxic prostate cancer cells independent of p53. Mol Cancer Ther. 2008 Apr;7(4):993-9.
单位
1mM-5mg8.5986mL
1mM-1mg1.7197mL
1mM-10mg17.1972mL
5mM-1mg0.3439mL
5mM-5mg1.7197mL
5mM-10mg3.4394mL
10mM-1mg0.172mL
10mM-5mg0.8599mL
10mM-10mg1.7197mL

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