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  • 化合物 666-15|T5318|TargetMol

化合物 666-15|T5318|TargetMol

666-15
1433286-70-4
413 1mg 起订
945 5mg 起订
1530 10mg 起订
上海 更新日期:2024-12-12

TargetMol中国(陶术生物)

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联系人:邵小姐
手机:4008200310 拨打
邮箱:marketing@tsbiochem.com

产品详情:

中文名称:
化合物 666-15
英文名称:
666-15
CAS号:
1433286-70-4
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格:
99.77%
产品类别:
抑制剂
货号:
T5318

Product Introduction

Bioactivity

名称666-15
描述666-15 is a selective CREB inhibitor with an IC50 of 81 nM. 666-15 can effectively inhibit the growth of breast cancer.
细胞实验HEK 293T cells in a 10 cm plate were transfected with pCRE-RLuc (6 μg) with Lipofectamine2000 following the manufacturer's instructions. Three hours after transfection, the cells were collected and replated into 96-well plates at ~10?000 cells/well. The cells were allowed to attach to the bottom of the plates overnight. The cells were then treated with different concentrations of different compounds for 30 min when forskolin (10 μM) was added to each well. The cells were incubated for further 5 h before cell lysis using 1× 30 μL Renilla luciferase lysis buffer. An amount of 5 μL of the lysate was combined with 30 μL of benzyl-coelenterazine solution in PBS (pH 7.4, 10 μg/mL). The protein concentration in each well was determined. The Renilla luciferase activity was normalized to protein content in each well and expressed as relative luciferase unit/μg protein (RLU/μg protein). The IC50 was derived from nonlinear regression analysis of the RLU/μg protein–concentration curve [1].
动物实验Each 6- to 8-week old BALB/c nude mouse was inoculated subcutaneously at the right flank with MDA-MB-468 cells (5 × 10^6) in 0.1 mL of HBSS with Matrigel (1:1) for tumor development. When the tumor volume reached approximately 100 mm3, the mice were randomized to be treated with either vehicle or 666-15 at 10 mg/kg. 3i was dissolved in 1% N-methylpyrrolidone (NMP), 5% Tween-80 in H2O. The dosing solution was prepared weekly. The mice were treated once a day for 5 consecutive days a week, and the treatment lasted for 5 weeks. During the treatment, the tumor size and body weight were measured 2–3 times a week. The tumors were measured in two dimensions using a digital caliper, and the volume was expressed in mm3 using the formula V = 0.5ab2, where a and b represent the long and short diameters of the tumor, respectively. The tumor volume was normalized to the initial tumor volume at the time of the first treatment [1].
体外活性方法:666-15浓度为62.5至500nM处理OA 样软骨细胞,研究 666-15 对 OA 样老年豚鼠软骨细胞的活力。 结果:p-CREB1蛋白水平显著降低,并显著提高老年豚鼠软骨细胞的细胞活力。[1] 方法:为了研究CREB抑制的生物学效应,将SySa细胞与浓度增加(0.13-5μM)的666-15一起孵育并进行在MTT测定。 结果:666-15以剂量依赖性方式显着抑制SySa细胞活力(IC50:0.36-1.72 μM)。[2]
体内活性方法:小鼠被随机分配到不同组别,包括正常组、假手术组、ACLT+溶剂对照组、以及两个不同剂量的666-15处理组(ACLT+666-15低剂量组,5 mg/kg;ACLT+666-15高剂量组,10 mg/kg,腹腔注射,每周一次,六周)。 结果:666-15治疗能缓解关节退变,降低软骨中降解标志物如CTX-II的水平,减轻滑膜炎症,且不影响小鼠体重,表明其安全性。[1]
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 60 mg/mL (96.7 mM)
关键字breast | Epigenetic Reader Domain | cancer | CREB | 66615 | 666-15 | 666 15 | inhibit | Inhibitor
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CREB inhibitor|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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