伏拉塞替三盐酸盐|T41100|TargetMol

价格	￥10600
包装	25mg

最小起订量	1mg
发货地	上海
更新日期	2024-09-29

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产品详情

中文名称:伏拉塞替三盐酸盐	英文名称:Volasertib trihydrochloride
CAS:946161-17-7	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.
产品类别: 抑制剂
货号: T41100

Product Introduction

Bioactivity

名称	Volasertib trihydrochloride
描述	Volasertib (BI 6727) trihydrochloride is a dihydropteridinone derivative that exhibits potent and selective inhibition of Polo-like kinase 1 (PLK1), PLK2, and PLK3. It acts as an orally active ATP-competitive inhibitor with an IC50 of 0.87 nM against PLK1. Additionally, Volasertib trihydrochloride demonstrates IC50 values of 5 nM and 56 nM against PLK2 and PLK3, respectively. Its mechanism of action includes inducing mitotic arrest and apoptosis. Furthermore, Volasertib trihydrochloride has been shown to possess significant antitumor activity in various cancer models.
体外活性	Volasertib trihydrochloride (BI 6727 trihydrochloride; 0.01-10000 nM; 72 hours) has EC 50 values of 11 to 37 nmol/L in multiple cell lines[1]. Volasertib trihydrochloride (10-1000 nM; 24 hours) results accumulation of cells with 4N DNA content, indicative of a cell cycle block in G2-M phase[1]. Volasertib trihydrochloride (100 nM; 24-72 hours) induces cell apoptosis at 48 hours[1]. Cell Proliferation Assay[1]Cell Line: Multiple cell lines Concentration: 0.01-10000 nM Incubation Time: 72 hours Result: Inhibited proliferation of multiple cell lines derived from various cancer tissues, including carcinomas of the colon (HCT 116, EC 50 =23 nmol/L) and lung (NCI-H460, EC 50 =21 nmol/L), melanoma (BRO, EC 50 =11 nmol/L), and hematopoietic cancers (GRANTA-519, EC 50 =15 nmol/L; HL-60, EC 50 =32 nmol/L; THP-1, E 50 =36 nmol/L and Raji, EC 50 =37 nmol/L) with EC 50 values of 11 to 37 nmol/L. Apoptosis Analysis[1]Cell Line: NCI-H460 cells Concentration: 100 nM Incubation Time: 24, 48, 72 hours Result: G2-M arrest at 24 hours was followed by induction of apoptosis at 48 hours. Cell Cycle Analysis[1]Cell Line: NCI-H460 cells Concentration: 10, 30, 100, 300, 1000 nM Incubation Time: 24 hours Result: Resulted in accumulation of cells with 4N DNA content, indicative of a cell cycle block in G2-M phase.
体内活性	Volasertib trihydrochloride (BI 6727 trihydrochloride; A total weekly dose of 50 mg/kg; Oral; once a week, twice a week, or daily; for 40 days) shows comparable efficacy in human colon carcinoma xenograft models[1]. Volasertib trihydrochloride (15, 20, or 25 mg/kg/day; i.v.; 2 consecutive days per week; for 40 days) leads to significant tumor growth delay and even tumor regression in human colon carcinoma xenograft models[1]. Volasertib trihydrochloride (70 mg/kg given once weekly or 10 mg/kg daily; oral) significantly delays tumor growth in a non-small cell lung carcinoma xenograft model derived from NCI-H460 cells[1]. Volasertib (a single dose of 40 mg/kg; iv) causes a significant (13-fold) increase in mitotic cells in HCT 116 tumor-bearing nude mice[1]. Volasertib has high volume of distribution and a long terminal half-life in mice (V ss =7.6 L/kg, t 1/2 =46 h) and rats (V ss =22 L/kg, t 1/2 =54 h)[1]. Animal Model: Female BomTac:NMRI-Foxn1 nu mice (Taconic) were grafted s.c. with HCT 116 human colon carcinoma cells (ATCC CCL-247)[1]Dosage: A total weekly dose of 50 mg/kg Administration: Oral; once a week, twice a week, or daily; for 40 days Result: Showed comparable efficacy and were well tolerated. Animal Model: Female BomTac:NMRI-Foxn1 nu mice and male Wistar rats of the strain Crl:WI[1]Dosage: 35 mg/kg (mice) or 10 mg/kg (rat) (Pharmacokinetic Analysis) Administration: IV 5-minute infusion; a single dose 5-minute infusion Result: Had high volume of distribution and a long terminal half-life in mice (V ss =7.6 L/kg, t 1/2 =46 h) and rats (V ss =22 L/kg, t 1/2 =54 h).
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
关键字	Volasertib \| Volasertib Trihydrochloride \| Volasertib trihydrochloride

关键字： BI6727trihydrochloride|||伏拉塞替三盐酸盐|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	2013-04-18 （12年）	注册资本	589.8595万人民币
员工人数	100-500人	年营业额	￥ 1亿以上
主营行业	中间体,天然产物,生物化工,化学试剂,生物技术服务	经营模式	贸易,工厂,试剂,定制,服务

TargetMol中国（陶术生物）

VIP 1年

公司成立：12年
注册资本：589.8595万人民币
企业类型：有限责任公司(自然人投资或控股)
主营产品：抑制剂&激动剂，天然产物，重组蛋白，化合物库，技术服务
公司地址：上海市静安区江场三路238号8楼

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