UNBS 5162
目录号 : GC17538
A antagonist of CXCL chemokine expression
Cas No.:956590-23-1
Sample solution is provided at 25 µL, 10mM.
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UNBS5162 is a pan-antagonist of CXCL chemokines. By using the MTT colorimetric assay, IC50 values of the mean antiproliferative activity against nine human cancer cell lines were 19.8 and 17.9 μ M for UNBS3157 and UNBS5162, respectively.
CXCL chemokines is composed of a CXC chemokine domain, a mucin-like stalk, a transmembrane domain and a cytoplasmic tail containing a potential tyrosine phosphorylation site that may bind SH2.
UNBS5162 display weak antiproliferative activity in vitro.
UNBS5162 increases the therapeutic benefits of taxol in the orthotopic human PC-3 prostate cancer model. The proliferation of PC-3 cell and DU-145 prostate cancer cells were prevented by 10 μM UNBS5162 in vitro after the 6-day treatment. Flow cytometry analysis revealed that treatment of PC-3 and DU-145 cells with 10 μM UNBS5162 for 72 hours markedly blocked PC-3 cells in their G2 cell cycle phase and to a lesser extent in DU-145 cells. The percentage of PC-3 cells in the G2/M phase markedly increased, and accordingly the percentage of cells in the G1 phase diminished. The Rb protein expression in PC-3 cells was completely abolished after 48 and 72 hours treatment of 10 μM UNBS5162.
The cell cycle kinetics of PC-3 or DU-145 was not significantly modified by 1 μM UNBS5162. UNBS5162 at 1 μM induced no marked modifications in Rb, pRb, and E2F1 protein expression. UNBS5162 at concentrations higher than 1 μM was toxic, as indicated by inhibited proliferation of murine and human hematopoietic stem and progenitor cells
References:
[1]. Mijatovic T, Mahieu T, Bruyère C et al. UNBS5162, a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers. Neoplasia. 2008 Jun;10(6):573-86.
Animal experiment: | Mice[1]Orthotopic xenografts are obtained by injecting 2.5 × 106 human PC-3 or DU-145 cells into the prostate of 6-week-old male nu/nu mice (n = 9 animals per treatment group). All grafts are performed under anesthesia [saline/Rompun/Imalgene; 5:1:1 by volume]. The end point in these orthotopic experiments is the survival period of the tumor-bearing mice after the administration of UNBS3157, UNBS5162, or reference anticancer agents (taxol, mitoxantrone, and amonafide). However, for ethical reasons, animals are killed when 20% of body weight have been lost compared to that determined at the time of tumor grafting. All animals are weighed three times a week. Autopsies and histologic diagnoses are performed on each mouse to confirm the presence of tumor development; 100% is achieved. In the case of UNBS5162 experiments in the PC-3 model, after the sacrifice of animals, tumors are removed from both drug-treated [10 mg/kg, intravenous (i.v.)] and vehicle-treated mice, fixed in buffered formalin, embedded in paraffin, and 5-µm-thick sections taken. These histologic slides are then stained with hematoxylin and eosin for blood vessel counts[1]. |
References: [1]. Mijatovic T, et al. UNBS5162, a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers. Neoplasia. 2008 Jun;10(6):573-86. | |
| Cas No. | 956590-23-1 | SDF | |
| 化学名 | 1-(2-(2-(dimethylamino)ethyl)-1,3-dioxo-2,3-dihydro-1H-benzo[de]isoquinolin-5-yl)urea | ||
| Canonical SMILES | CN(C)CCN1C(C2=C3C(C=CC=C3C1=O)=CC(NC(N)=O)=C2)=O | ||
| 分子式 | C17H18N4O3 | 分子量 | 326.35 |
| 溶解度 | DMF: 3 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 2 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0642 mL | 15.321 mL | 30.6419 mL |
| 5 mM | 0.6128 mL | 3.0642 mL | 6.1284 mL |
| 10 mM | 0.3064 mL | 1.5321 mL | 3.0642 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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