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  • 化合物 LB42708|T2678|TargetMol

化合物 LB42708|T2678|TargetMol

LB42708
226929-39-1
262 1mg 起订
368 2mg 起订
697 5mg 起订
上海 更新日期:2024-09-30

TargetMol中国(陶术生物)

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联系人:邵小姐
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邮箱:marketing@tsbiochem.com

产品详情:

中文名称:
化合物 LB42708
英文名称:
LB42708
CAS号:
226929-39-1
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:
97.83%
产品类别:
抑制剂
货号:
T2678

Product Introduction

Bioactivity

NameLB42708
DescriptionLB42708 is an orally active farnesyltransferase (FTase) inhibitor (IC50: 0.8/1.2/2.0 nM toward H/N/K-ras).
Cell ResearchCell growth is measured by MTT. Briefly, cells were seeded at 2 × 103 cells per well in 96-well culture plates in triplicate. After the addition of various concentrations of drugs, cells are incubated for 72 h. At the end of culture, the plates are washed twice with PBS, and cells are incubated with 200 μl of RPMI 1640 containing 10% FCS and 0.25 mg/ml of MTT at 37 °C for 3 h. The absorbance of each well is measured with Titer-Tech 96-well multiscanner at 570 nm. The viable cell number is proportional to the absorbance. (Only for Reference)
Kinase AssayBiochemical Assessment of PDGFRα Kinase Activity: Chinese hamster ovary (CHO) cells are transiently transfected with mutated or wild type PDGFRα constructs and treated with various concentrations of Crenolanib. Experiments involving recombinant DNA are performed using biosafety level 2 conditions in accordance with guidelines. Protein lysates from cell lines are prepared and subjected to immunoprecipitation using anti-PDGFRα antibodies followed by sequential immunoblotting for PDGFRα. Densitometry is performed to quantify drug effect using Photoshop software, with the level of phosphor- PDGFRα normalized to total protein. Densitometry and proliferation experimental results are analyzed using Calcusyn 2.1 software to mathematically determine the IC50 values. The Wilcoxon Rank Sum Test is used to compare the IC50 values of Crenolanib for a given mutation.
In vitro在脂多糖的小鼠中, LB42708(12.5 mg/kg,i.p.)抑制NO、前列腺素E2、TNF-α及IL-1β的产生,并抑制CIA的进程.在Ras野生型和突变型的肿瘤中,LB42708(20 mg/kg/day,i.p.)对肿瘤生长及血管新生有抑制作用.
In vivo在H-ras和K-ras-改变的大鼠肠内壁细胞中,LB42708对生长和诱导凋亡有不可逆的抑制作用。在肿瘤相关的内皮细胞中,通过阻断Ras依赖的MAPK 和PI3K/Akt信号通路,LB42708对VEGF诱导的肿瘤血管新生产生抑制作用。在鼠巨噬细胞系RAW264.7细胞中,LB42708对脂多糖 + IFN-γ诱导的细胞内法尼化蛋白p21ras过程有明显抑制作用。在免疫激活的成骨细胞和巨噬细胞中,LB42708抑制一氧化氮合酶、环氧合酶-2、TNF-α及IL-1β、NO和PGE(2)的产生。通过抑制IKK活性,LB42708对NF-κB激活和iNOS启动子活性产生抑制作用。
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationEthanol : 55.6 mg/mL (100 mM)
DMSO : 45 mg/mL (81.01 mM), Sonication is recommended.
KeywordsFtase | Apoptosis | Inhibitor | H-Ras | orally active | K-Ras4B | N-Ras | LB42708 | Farnesyl Transferase | inhibit | LB-42708 | farnesyltransferase inhibitor | LB 42708
Inhibitors RelatedRisedronate Sodium | Alendronate sodium hydrate | OU749 | Entacapone | Risedronic Acid | 3-Methoxybenzamide | Minodronic acid monohydrate | Serotonin hydrochloride | Flopropione | Testosterone propionate | Ibandronate sodium | (E)-Daporinad
Related Compound LibrariesInhibitor Library | Bioactive Compound Library | Bioactive Compounds Library Max
LB42708|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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