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Volasertib trihydrochloride
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 trihydrochloride图片
CAS NO:946161-17-7
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
伏拉塞替三盐酸盐
BI 6727 trihydrochloride
产品介绍
Volasertib (BI 6727) trihydrochloride 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 trihydrochloride 抑制 PLK2 和 PLK3,IC50分别为 5 和 56 nM。Volasertib trihydrochloride 诱导有丝分裂停滞和细胞凋亡。Volasertib trihydrochloride 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) trihydrochloride is an orally active, highly potent and ATP-competitivePolo-like kinase1 (PLK1)inhibitor with anIC50of 0.87 nM. Volasertib trihydrochloride inhibitsPLK2andPLK3withIC50s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest andapoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiplecancermodels[1][2].

IC50& Target[1]

PLK1

0.87 nM (IC50)

PLK2

5 nM (IC50)

PLK3

56 nM (IC50)

体外研究
(In Vitro)

Volasertib trihydrochloride (BI 6727 trihydrochloride; 0.01-10000 nM; 72 hours) has EC50values 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, 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 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 (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

728.20

Formula

C34H53Cl3N8O3

CAS 号

946161-17-7

中文名称

伏拉塞替三盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.