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网站主页 化工产品目录 生物化工 抑制剂 丝裂原活化蛋白激酶(MAPK) Raf 抑制剂 TAK-632 化合物 TAK632
  • 化合物 TAK632|T1886|TargetMol

化合物 TAK632|T1886|TargetMol

TAK-632
1228591-30-7
326 2mg 起订
541 5mg 起订
827 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
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邮箱:marketing@tsbiochem.com

产品详情:

中文名称:
化合物 TAK632
英文名称:
TAK-632
CAS号:
1228591-30-7
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:
98.92%
产品类别:
抑制剂
货号:
T1886

Product Introduction

Bioactivity

名称TAK-632
描述TAK-632 is a potent pan-Raf inhibitor.
细胞实验The cells are proliferated in appropriate medium (vender recommended) supplemented with 10% heat-inactivated fetal bovine serum (FBS) and antibiotics, in tissue culture dishes placed in a humidified incubator maintained at 37°C in an atmosphere of 5% CO2 and 95% air. The anti-proliferative activity of compound is determined by treating cell lines with the compound for 3 days, followed by measurement of viable cell number in the Cell Titer-Glo assay. The cells are seeded in a 96-multiwell plate at 1500 to 4000 cells per well in medium containing FBS and cells allowed to sit down overnight. After 18–20 h, compounds at various concentrations by serial dilution are added to the cells and were cultured for 3 days in chamber. After the treatment culture, cellular proliferation is determined by a Cell Titer-Glo Luminescent Cell Viability Assay. In brief, 100 bL/well of Cell Titer-Glo Substrate solution is added to each well and the cells were cultured for an additional 10 minutes (approximately). The chemi-luminescence value is measured using a Luminescence Counter 1420 ARVO MX Light. Concentration response curves are generated by calculating the decrease in chemi-luminescence values in compound-treated samples relative to the vehicle (DMSO) treated controls. (Only for Reference)
激酶实验Kinase Profile Assay: Assays for serine/threonine kinases using radio labeled [γ-33P] ATP are performed in 96 well plates. BRAF and c-RAF are expressed as N-terminal FLAG-tagged protein using a baculovirus expression system. The reaction conditions are optimized for each kinase: BRAF (25 ng/well of enzyme, 1 μg/well of GST-MEK1(K96R), 0.1 μCi/well of [γ-32P] ATP, room temperature, 20 min reaction); c-RAF (25 ng/well of enzyme, 1 μg/well of GST-MEK1 (K96R), 0.1 μCi/well of [γ-32P] ATP, room temperature, 20 min reaction). Enzyme reactions are performed in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol and 0.5 μM ATP containing optimized concentration of enzyme, substrate and radiolabeled ATP as described above in a total volume of 50 μL. Prior to the kinase reaction, compound and enzyme are incubated for 5 min at reaction temperature as described above. The kinase reactions are initiated by adding ATP. After the reaction period as described above, the reactions are terminated by the addition of 10% (final concentration) trichloroacetic acid. The [γ-33P] or [γ-32P]-phosphorylated proteins are filtered in GFC filter plates with a Cell Harvester and then the plates are washed out with 3% phosphoric acid. The plates are dried, followed by the addition of 40 μL of MicroScint0. The radioactivity is counted by a TopCount scintillation counter.
体外活性在携带NRAS突变型黑素瘤的SK-MEL-2异种移植小鼠模型中,口服 TAK-632(60 or 120 mg/kg)抑制 MAPK 信号通路,抑制肿瘤的发展.
体内活性在A375(GI50=66 nM)和HMVII系(和GI50=200 nM)中,TAK-632能够抑制细胞增殖。其中,在黑色素瘤A375细胞系(BRAFV600E)中,TAK-632抑制MEK(IC50=2 nM)和ERK磷酸化(IC50=16 nM)。在人类黑色素瘤HMVII细胞系(NRASQ61K/BRAFG469V)中,TAK-632抑制pMEK(IC50=49 nM)和pERK(IC50=50 nM)。
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 : 93 mg/mL (167.7 mM)
Ethanol : 2 mg/mL (3.6 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字inhibit | Inhibitor | TAK632 | Raf kinases | TAK-632 | Raf | Aurora Kinase | TAK 632
相关产品Imatinib | Amlexanox | Dabrafenib | Formononetin | Axitinib | Lenvatinib mesylate | Ferulic Acid | Regorafenib | Pazopanib | Nintedanib | Sorafenib | Regorafenib monohydrate
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TAK-632|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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