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Volasertib

BI-6727,BI 6727,BI6727

Volasertib(BI6727)是高活性PLK1抑制剂,IC50为0.87 nM,比对Plk2和Plk3的抑制性高6倍和65倍。

目录号
EY1331
EY1331
EY1331
EY1331
纯度
99.66%
99.66%
99.66%
99.66%
规格
1 mg
5 mg
10 mg
50 mg
原价
360
860
1400
4700
售价
360
860
1400
4700
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Volasertib (BI 6727) is a highly potent Plk1 inhibitor with IC50 of 0.87 nM in a cell-free assay. It shows 6- and 65-fold greater selectivity against Plk2 and Plk3. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 AKm系数


    例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。


  • 参考文献

    [1] Rudolph D, et al. Clin Cancer Res, 2009, 15(9), 3094-3102.

    分子式
    C34H50N8O3
    分子量
    618.81
    CAS号
    755038-65-4
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    20 mg/mL
    Water
    <1 mg/mL
    Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01662505 Leukemia, Myeloid, Acute Drug: Volasertib Boehringer Ingelheim Phase 1 2012-08-01 2015-07-30
    NCT01348347 Neoplasms Drug: Volasertib, low dose, d1q3w|Drug: Volasertib, middle dose, d1q3w|Drug: Volasertib, high dose, d1q3w Boehringer Ingelheim Phase 1 2011-04-01 2014-08-06
    NCT02722135 Leukemia, Myeloid, Acute Drug: Volasertib Boehringer Ingelheim Phase 1 2016-11-01 2017-01-26
    NCT02003573 Leukemia, Myeloid, Acute Drug: decitabine iv|Drug: volasertib iv infusion Boehringer Ingelheim Phase 1 2014-01-01 2016-12-14
    NCT01145885 Neoplasms Drug: BI 6727 Boehringer Ingelheim Phase 1 2010-06-01 2013-10-31
    NCT01772563 Neoplasms Drug: volasertib|Drug: itraconazole Boehringer Ingelheim Phase 1 2013-02-01 2017-02-14
    NCT02905994 AML Drug: Volasertib|Drug: Cytarabine|Drug: Idarubicin|Procedure: Bone Marrow Biopsy Massachusetts General Hospital|Boehringer Ingelheim Phase 1 2016-09-01 2017-02-15
    NCT02527174 Leukemia, Myeloid, Acute|Leukemia, Monocytic, Acute|Leukemia, Myelomonocytic, Acute|Leukemia, Erythroblastic, Acute|Leukemia, Megakaryoblastic, Acute Drug: Volasertib|Drug: Idarubicin|Drug: Cytarabine University of Alberta Phase 1 2016-11-01 2016-10-26
    NCT02861040 Recurrent Adult Acute Lymphoblastic Leukemia|Refractory Adult Acute Lymphoblastic Leukemia Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Vincristine Sulfate Liposome|Drug: Volasertib Northwestern University|National Comprehensive Cancer Network|National Cancer Institute (NCI) Phase 1 2016-08-01 2016-12-13
    NCT00969761 Neoplasms Drug: BI-6727|Drug: BI 6727 Boehringer Ingelheim Phase 1 2009-08-01 2012-07-25
    NCT02201329 Myelodysplastic Syndromes|Leukemia, Myelomonocytic, Chronic Drug: Azacitidine|Drug: Volasertib Boehringer Ingelheim Phase 1 2014-08-01 2015-09-30
    NCT02875002 Relapsed and Refractory Aggressive B- and T-cell Lymphomas|Lymphoma Drug: volasertib|Drug: belinostat Yale University|Massey Cancer Center|Sidney Kimmel Comprehensive Cancer Center Phase 1 2016-10-01 2016-08-23
    NCT02721875 Myelodysplastic Syndromes Drug: Volasertib|Drug: Volasertib|Drug: Azacitidine Boehringer Ingelheim Phase 1 2016-04-01 2016-12-19
    NCT02198482 Acute Myeloid Leukemia (AML)|High-risk Myelodysplastic Syndrome (MDS) Drug: Volasertib|Drug: Cytarabine|Drug: Daunorubicin|Drug: Mitoxantrone University of Ulm Phase 2 2016-02-01 2016-12-02
    NCT02757248 PTCL|CTCL Drug: Volasertib|Drug: Romidepsin Anne Beaven, MD|National Comprehensive Cancer Network|Boehringer Ingelheim|Duke University Phase 1 2016-11-01 2016-11-29
    NCT01022853 Neoplasms Drug: BI 6727|Drug: BIBF 1120 Boehringer Ingelheim Phase 1 2009-12-01 2013-11-01
    NCT01206816 Neoplasms Drug: BI 6727 + BIBW 2992 Boehringer Ingelheim Phase 1 2010-10-01 2013-10-31
    NCT01957644 Myelodysplastic Syndromes|Leukemia, Myelomonocytic, Chronic Drug: Azacitidine|Drug: Volasertib Boehringer Ingelheim Phase 1 2013-11-01 2017-01-10
    NCT00824408 Carcinoma, Non-Small-Cell Lung Drug: pemetrexed|Drug: pemetrexed|Drug: BI 6727 Boehringer Ingelheim Phase 2 2009-03-01 2016-07-28
    NCT00804856 Leukemia, Myeloid, Acute Drug: BI 6727 (d1 and 15)|Drug: BI 6727 (d1 and 15)|Drug: Cytarabine|Drug: Cytarabine Boehringer Ingelheim Phase 2 2008-11-01 2016-08-22
    NCT01721876 Leukemia, Myeloid, Acute Drug: placebo|Drug: volasertib|Drug: low dose cytarabine|Drug: low dose cytarabine Boehringer Ingelheim Phase 3 2013-01-01 2016-08-22

    注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。

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