伏拉塞替|T6019

Volasertib
755038-65-4

￥397 2mg 起订

￥679 5mg 起订

￥1070 10mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 伏拉塞替

英文名称：: Volasertib

CAS号：: 755038-65-4

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：: 99.72%

产品类别：: 抑制剂

货号：: T6019

Product Introduction

Bioactivity

名称	Volasertib
描述	Volasertib (BI 6727) (BI-6727) is a potent inhibitor of PLK1 (IC50: 0.87 nM), inducing mitotic arrest and apoptosis. It also inhibits PLK2/PLK3 (IC50s: 5/56 nM).
细胞实验	Cell proliferation assays were done by incubating cells in the presence of various concentrations of BI 6727 for 72 h and cell growth was assessed by measuring Alamar blue dye conversion in a fluorescence spectrophotometer. Effective concentrations at which cellular growth was inhibited by 50% (EC50) were extrapolated from the dose-response curve fit [1].
激酶实验	Recombinant human Plk1 (residues 1-603) was expressed as NH2-terminal, GST-tagged fusion protein using a baculoviral expression system and purified by affinity chromatography using glutathione-agarose. Enzyme activity assays for Plk1, Plk2, and Plk3 were done in the presence of serially diluted inhibitor using 20 ng of recombinant kinase and 10 μg casein from bovine milk as substrate. Kinase reactions were done in a final volume of 60 μL for 45 min at 30°C [15 mmol/L MgCl2, 25 mmol/L MOPS (pH 7.0), 1 mmol/L DTT, 1% DMSO, 7.5 μmol/L ATP, 0.3 μCi γ-32P-ATP]. Reactions were terminated by the addition of 125 μL of ice-cold 5% TCA. After transferring the precipitates to MultiScreen mixed ester cellulose filter plates, plates were washed with 1% TCA and quantified radiometrically. Dose-response curves were used for calculating IC50 values. To establish a kinase selectivity profile, additional kinase assays were done by contract research organizations or reagents were purchased from commercial sources and assays were done according to the supplier's instructions. Appropriate positive and negative controls were included in the assay design [1].
动物实验	Female BomTac:NMRI-Foxn1nu mice were grafted s.c. with 2 × 10^6 HCT 116 human colon carcinoma cells (ATCC CCL-247), 1 × 10^6 NCI-H460 non–small cell lung cancer cells (ATCC HTB-177), or CXB1 human colon carcinoma tumor pieces derived from patient material by serial transplantation in nude mice. When tumors had reached a volume of ～50 to 100 mm^3, animals were randomized into treatment and control groups of 10 mice each. BI 6727 was formulated in hydrochloric acid (0.1 N), diluted with 0.9% NaCl, and injected i.v. into the tail vein at the indicated dose and schedule. For oral treatment, BI 6727 was resuspended in 0.5% Natrosol 250 hydroxyethyl-cellulose and given intragastrally via gavage needle. An administration volume of 10 mL per kilogram of body weight was used for both administration routes. Tumor volumes were determined thrice a week using a caliper. The results were converted to tumor volume (mm^3) by the formula length × width2 × π/6. The weight of the mice was determined as an indicator of tolerability on the same days. Median tumor volumes on the last day of the experiment were used to calculate treated versus control values (= tumor volume treated mice × 100/tumor volume control mice) [1].
体外活性	Volasertib（BI 6727）有效抑制了Plk1及其两个密切相关的激酶Plk2和Plk3（IC50值分别为0.87、5、56 nmol/L）。BI 6727能够抑制来自多种癌症组织的多种细胞系的增殖，包括结肠癌（HCT 116，EC50=23 nmol/L）和肺癌（NCI-H460，EC50=21 nmol/L），黑色素瘤（BRO，EC50=11 nmol/L）以及血液癌症（GRANTA-519，EC50=15 nmol/L；HL-60，EC50=32 nmol/L），其EC50值范围为11至37 nmol/L [1]。BI 6727对NB TICs显示出nM级别的活性，EC50为21 nmol/L，并具有出色的选择性，SKPs的EC50为2.8 μmol/L [2]。在测试的所有40种细胞系中，Volasertib抑制了增殖，平均半最大抑制浓度为313 nmol/l（范围：4-5000 nmol/l）[3]。
体内活性	BI 6727具有良好的理化性质和药代动力学性质，能够进行静脉注射(i.v.)以及口服制剂的体内测试，为给药计划提供了灵活性。此外，BI 6727在多种癌症模型中显示出显著的抗肿瘤活性，包括对紫杉醇耐药性结肠癌模型[1]。Volasertib对RMS-1泡状肌肉瘤移植瘤表现出高度活性，实现了100%的肿瘤消退。其活性与G2/M期阻滞的完全和持久相关，并随后引起凋亡细胞死亡。Volasertib与长春新碱表现出协同作用，但与依托泊苷表现出拮抗效应[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	H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 14 mg/mL (22.62 mM), Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble)
关键字	GRANTA-519 \| Raji \| BRO \| Inhibitor \| ATP-competitive \| Volasertib \| mitotic \| HL-60 \| BI-6727 \| orally \| Polo-like Kinase (PLK) \| HCT 116 \| arrest \| NCI-H460 \| inhibit \| BI6727 \| dihydropteridinone \| Apoptosis \| THP-1
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 \| 抗癌活性化合物库 \| 抗癌上市药物库 \| 经典已知活性库 \| 抗衰老化合物库 \| FDA 上市激酶抑制剂库 \| 药物功能重定位化合物库 \| 抗癌药物库

伏拉塞替|||BI 6727|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子