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。
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.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km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。
[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
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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