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网站主页 化工产品目录 生物化工 抑制剂 细胞周期(Cell Cycle) Aurora Kinase 抑制剂 5-[[7-[3-[乙基(2-羟基乙基)氨基]丙氧基]-4-喹唑啉]氨基]-N-(3-氟苯基)-1H-吡唑-3-乙酰胺 化合物 Barasertib
  • 化合物 Barasertib|T2602|TargetMol

化合物 Barasertib|T2602|TargetMol

Barasertib-HQPA
722544-51-6
339 2mg 起订
498 5mg 起订
698 10mg 起订
上海 更新日期:2024-12-12

TargetMol中国(陶术生物)

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产品详情:

中文名称:
化合物 Barasertib
英文名称:
Barasertib-HQPA
CAS号:
722544-51-6
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:
99.29%
产品类别:
抑制剂
货号:
T2602

Product Introduction

Bioactivity

名称Barasertib-HQPA
描述Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor (IC50: 0.37 nM) and demonstrates ~3,700-fold greater selectivity than Aurora A.
细胞实验LNCaP cells were cultured in RPMI 1640 medium supplemented with 10 % fetal bovine serum, in 5 % CO2 at 37 °C. The cells were treated with 5, 10, 50, 100, and 500 nM of AZD1152-HQPA for 48 h. After 48-h treatment with AZD1152-HQPA, cells were further incubated with 100 μl of MTT (0.5 mg/ml) at 37 °C for 2 h. Precipitated formazan was solubilized with 100 μl of DMSO, and the optical densitometry was measured at a wavelength of570 nm. Cell treated with 0.1 % DMSO was defined as the control group [2].
动物实验Female immune-deficient BALB/c nude mice at 4 weeks of age were maintained in pathogen-free conditions with irradiated chow. Animals were bilaterally, subcutaneously injected with 2 × 10^6 MOLM13 cells/tumor in 0.1 mL Matrigel. When MOLM13 cells formed palpable tumors, mice were divided randomly into control (n=5) and treatment groups (n=5), and treatment was begun. AZD1152 (5 or 25 mg/kg) with or without vincristine (0.2 mg/kg) was given to mice by intraperitoneal injection 4 times a week or every another day, respectively. Daunorubicin (1 mg/kg) was given to mice by intraperitoneal injection 6 times during 2 weeks of treatment either alone or in combination with AZD1152 (5 mg/kg). The dose of these agents was determined by our preliminary studies (data not shown). Control diluent was given to the untreated control mice. Body weight and tumors were measured twice a week. Tumor sizes were calculated by the formula: a × b × c, where "a" is the length, "b" is the width, and "c" is the height in millimeters. At the end of the experiment, animals were killed by CO2 asphyxiation and tumor weights were measured after their careful resection. Tumor tissue was collected for analysis [1].
体外活性Barasertib抑制了急性髓性白血病(AML)系列(HL-60, NB4, MOLM13)、急性淋巴性白血病(ALL)系列(PALL-2)、双表型白血病(MV4-11)、急性嗜酸性白血病(EOL-1)以及慢性髓性白血病爆发期K562细胞的增殖,其半抑制浓度(IC50)范围为3 nM至40 nM [1]。Barasertib-HQPA处理导致LNCaP细胞系的存活能力缺陷、多倍体以及细胞死亡,并降低了AR表达 [2]。
体内活性Barasertib对AML系列(HL-60, NB4, MOLM13)、ALL系列(PALL-2)、双表型白血病(MV4-11)、急性嗜酸性白血病(EOL-1)以及慢性髓性白血病危重期K562细胞的增殖抑制作用显著,IC50值介于3 nM至40 nM之间[1]。Barasertib-HQPA处理导致LNCaP细胞系存活能力受损、多倍体形成及细胞死亡。此外,Barasertib-HQPA治疗降低了AR表达[2]。Barasertib强力抑制了免疫缺陷小鼠中人类结肠、肺和血液肿瘤异种移植物的生长。在用Barasertib静脉治疗携带SW620结直肠肿瘤的无胸腺大鼠中,首先观察到组蛋白H3磷酸化的暂时抑制,随后细胞中4N DNA含量比对照组高出2.4倍,继而多倍体细胞比例增加[3]。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度Ethanol : 3 mg/mL (5.91 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 94 mg/mL (185.2 mM)
关键字colon | Inhibitor | Barasertib-HQPA | Apoptosis | Aurora Kinase | BarasertibHQPA | AZD 2811 | cancer | INH 34 | AZD1152-HQPA|AZD 2811 | leukemia | breast | inhibit | AZD1152-HQPA|AZD-2811 | lung | INH-34 | AZD-2811 | INH34 | Barasertib HQPA
相关产品L-Glutamic acid | Metronidazole | 5-Fluorouracil | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | Myricetin | Sorafenib | L-Ascorbic acid | Acetylcysteine | Salicylic acid | Sodium 4-phenylbutyrate
相关库抑制剂库 | 经典已知活性库 | 抗癌活性化合物库 | 已知活性化合物库 | 激酶抑制剂库 | 抗衰老化合物库 | 高选择性抑制剂库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库
Barasertib|||AZD2811|||AZD1152-HQPA|AZD2811|||AZD1152-HQPA|||1H-Pyrazole-3-acetamide|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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