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Volasertib trihydrochloride

产品编号 T41100 CAS 946161-17-7

别名: BI6727trihydrochloride, 伏拉塞替三盐酸盐

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.

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Volasertib trihydrochloride Chemical Structure

Volasertib trihydrochloride, CAS 946161-17-7

规格	价格/CNY		货期	数量
25 mg	￥ 10,600		6-8周

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Volasertib trihydrochloride 的其他形式现货产品:

Volasertib

其他形式的 Volasertib trihydrochloride:

Volasertib
现货

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生物活性

化学信息

存储 & 溶解度

产品描述	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).

别名	BI6727trihydrochloride, 伏拉塞替三盐酸盐
分子量	728.2
分子式	C34H53Cl3N8O3
CAS No.	946161-17-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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