2. Cell Cycle/DNA Damage Apoptosis
  3. Polo-like Kinase (PLK) Apoptosis
  4. Volasertib trihydrochloride

Volasertib trihydrochloride  (Synonyms: 伏拉塞替三盐酸盐; BI 6727 trihydrochloride)

目录号: HY-12137A
产品使用指南

摩尔计算器

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。

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Volasertib trihydrochloride Chemical Structure

Volasertib trihydrochloride Chemical Structure

CAS No. : 946161-17-7

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Volasertib trihydrochloride 的其他形式现货产品:

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Volasertib trihydrochloride 相关抗体

Top Publications Citing Use of Products

    Volasertib trihydrochloride purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2017;43(4):1472-1486.  [Abstract]

    The addition of Volasertib (0.5-1.5 µg/mL blunts the increase of the percentage of annexin-V-binding erythrocytes following glucose deprivation, an effect reaching statistical significance at 1 and 1.5 µg/mL Volasertib.

    查看 Polo-like Kinase (PLK) 亚型特异性产品:

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    PLK1 PLK2 PLK3 PLK4

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Volasertib (BI 6727) trihydrochloride is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib trihydrochloride inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models[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 EC50 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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Volasertib trihydrochloride 相关抗体:

    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 EC50 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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Female BomTac:NMRI-Foxn1nu 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-Foxn1nu 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 (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
    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.
    纯度 & 产品资料
    参考文献

    Volasertib trihydrochloride 相关分类

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    Keywords:

    Volasertib trihydrochloride946161-17-7BI 6727 trihydrochloride伏拉塞替三盐酸盐Polo-like Kinase (PLK)ApoptosisorallyATP-competitivemitoticarrestdihydropteridinoneHCT 116NCI-H460BROGRANTA-519HL-60THP-1RajiInhibitorinhibitorinhibit

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