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UNBS 5162

目录号: PC10669 纯度: ≥98%
CXCL趋化因子的泛拮抗剂,UNBS5162 是一种广谱的趋化因子配体 CXCL 拮抗剂,具有抗肿瘤活性。
CAS No. :956590-23-1
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中文名称
UNBS 5162
中文别名
N-[2-[2-(二甲基氨基)乙基]-2,3-二氢-1,3-二氧代-1H-苯[de]异喹啉-5-基]脲R;UNBS-5162 抑制剂;N-[2-[2-(二甲基氨基)乙基]-2,3-二氢-1,3-二氧代-1H-苯并[de]异喹啉-5-基]脲
英文名称
UNBS 5162
英文别名
UNBS-5162;[2-[2-(dimethylamino)ethyl]-1,3-dioxobenzo[de]isoquinolin-5-yl]urea;N-?[2-?[2-?(dimethylamino)?ethyl]?-?2,?3-?dihydro-?1,?3-?dioxo-?1H-?benz[de]?isoquinolin-?5-?yl]UreaR;UNBS 5162;UNBS5162
Cas No.
956590-23-1
分子式
C17H18N4O3
分子量
326.35
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
详情描述
CXCL趋化因子的泛拮抗剂,UNBS5162 是一种广谱的趋化因子配体 CXCL 拮抗剂,具有抗肿瘤活性。
生物活性

UNBS5162 is a pan-antagonist of CXCL chemokine expression, with anti-tumor activity.

性状

Solid

IC50 & Target[1][2]

CXCL

 

体外研究(In Vitro)

UNBS5162 is a pan-antagonist of CXCL chemokine expression and exhibits weak antiproliferative activity against human cancer cell lines with mean IC50 of 17.9 μM. UNBS5162 markedly impairs PC-3 tumor cell growth kinetics, without inducing senescence, whereas the reverse feature is observed with respect to DU-145 cells. UNBS5162 is cytotoxic to a range of human cancer cell lines including glioblastoma (Hs683 and U373MG), colorectal (HCT-15 and LoVo), non-small-cell lung (A549) and breast (MCF-7), with IC50s of 0.5-5 μM. UNBS5162 also markedly increases the levels of expression of LC3-I and LC3-II in human cancer cells. UNBS5162 displays no anti-topoisomerase II activity. Moreover, UNBS5162 induces cancer cell death through lysosomal membrane permeabilization (LMP) in PC3 prostate cancer cells but not in U373 glioblastoma cells, with this LMP process occurring as an UNBS5162-induced decrease in Hsp70 expression. UNBS5162 inhibits the proliferation of esophageal cancer squamous cells via the PI3K/AKT signaling pathway. UNBS5162 downregulates the protein expression of proteins associated with the PI3K/AKT signaling pathway, including the levels of phosphorylated (p)-AKT, p-mechanistic target of rapamycin kinase, ribosomal protein S6 kinase β1 and cyclin D1.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

UNBS5162 (20 mg/kg, i.v.) increases the therapeutic benefits of taxol in vivo in the orthotopic human PC-3 prostate cancer model.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
溶解度数据
体外研究: 

DMSO : 21.5 mg/mL (65.88 mM; Need ultrasonic and warming)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0642 mL 15.3210 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
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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, 6 months; -20°C, 1 month。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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