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Volasertib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Volasertib图片
CAS NO:755038-65-4
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
伏拉塞替
BI 6727
产品介绍
Volasertib (BI 6727) 是一种具有口服活性的、高效的、ATP 竞争性的 Polo 样激酶 1 (PLK1) 抑制剂,IC50为 0.87 nM。Volasertib 抑制 PLK2 和 PLK3,IC50分别为 5 和 56 nM。Volasertib 诱导有丝分裂停滞和细胞凋亡。Volasertib 是一种二氢蝶呤酮衍生物,在多种癌症模型中显示出显着的抗肿瘤活性。
生物活性

Volasertib (BI 6727) is an orally active, highly potent and ATP-competitivePolo-like kinase1 (PLK1)inhibitor with anIC50of 0.87 nM. Volasertib inhibitsPLK2andPLK3withIC50s of 5 and 56 nM, respectively. Volasertib induces mitotic arrest andapoptosis. Volasertib, a dihydropteridinone derivative, shows marked antitumor activity in multiplecancermodels[1][2].

IC50& Target[3]

PLK1

0.87 nM (IC50)

PLK2

5 nM (IC50)

PLK3

56 nM (IC50)

体外研究
(In Vitro)

Volasertib (BI 6727; 0.01-10000 nM; 72 hours) has EC50values of 11 to 37 nmol/L in multiple cell lines[1].
Volasertib (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 (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, EC50=23 nmol/L) and lung (NCI-H460, EC50=21 nmol/L), melanoma (BRO, EC50=11 nmol/L), and hematopoietic cancers (GRANTA-519, EC50=15 nmol/L; HL-60, EC50=32 nmol/L; THP-1, E50=36 nmol/L and Raji, EC50=37 nmol/L) with EC50values 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.
体内研究
(In Vivo)

Volasertib (BI 6727; 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 (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 (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 (Vss=7.6 L/kg, t1/2=46 h) and rats (Vss=22 L/kg, t1/2=54 h)[1].

Animal Model:Female BomTac:NMRI-Foxn1numice (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-Foxn1numice 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 (Vss=7.6 L/kg, t1/2=46 h) and rats (Vss=22 L/kg, t1/2=54 h).
Clinical Trial
分子量

618.81

性状

Solid

Formula

C34H50N8O3

CAS 号

755038-65-4

中文名称

伏拉塞替

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 50 mg/mL(80.80 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.6160 mL8.0800 mL16.1600 mL
5 mM0.3232 mL1.6160 mL3.2320 mL
10 mM0.1616 mL0.8080 mL1.6160 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.36 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: 2.08 mg/mL (3.36 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (3.36 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.36 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。