Volasertib | BI 6727 | PLK | AmBeed-信号通路专用抑制剂

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伏拉塞替 /Volasertib 98%

货号：A232139 同义名： BI 6727

Volasertib（BI 6727）是一种口服活性、高效和ATP竞争性的Polo样激酶1（PLK1）抑制剂，IC50为0.87 nM。它抑制PLK2和PLK3，IC50值分别为5 nM和56 nM，诱导有丝分裂停滞和凋亡。Volasertib是一种二氢蝶啶酮衍生物，在多种癌症模型中表现出显著的抗肿瘤活性。

Volasertib 化学结构
CAS号：755038-65-4

Volasertib 3D分子结构
CAS号：755038-65-4

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Volasertib 纯度/质量文件产品仅供科研

货号：A232139 标准纯度： 98% 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

PLK 亚型比较

产品名称	PLK1 ↓ ↑	PLK2 ↓ ↑	PLK3 ↓ ↑	PLK4 ↓ ↑	其他靶点	纯度
HMN-214	✔					99%+
SBE13 HCl	++++ PLK1, IC50: 200 pM					98%
Onvansertib	+++ PLK1, IC50: 2 nM					99%+
Volasertib	++++ PLK1, IC50: 0.87 nM					98%
GSK461364	+++ PLK1, Ki: 2.2 nM					99%+
MLN0905	+++ PLK1, IC50: 2 nM					99%+
Ro3280	++ PLK1, IC50: 3 nM					99%
(E/Z)-Rigosertib sodium	+ PLK1, IC50: 9 nM	+ PLK2, IC50: 260 nM			Bcr-Abl	99%+
BI 2536	++++ PLK1, IC50: 0.83 nM	++ PLK2, IC50: 3.5 nM	+ PLK3, IC50: 9.0 nM			99%+
CFI-400945				++ PLK4, IC50: 2.8 nM	Tie-2	98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Volasertib 生物活性

靶点	PLK1 PLK1, IC50:0.87 nM
描述	BI 6727 is a highly potent PLK inhibitor with IC50 values of 0.87nM, 5nM and 56nM for PLK1, 2 and 3, respectively. Volasertib inhibited proliferation of multiple cell lines with EC50 values of 23nM, 21nM, 11nM, 15nM, 32nM, 36nM and 37nM for HCT 116, NCI-H460, BRO, GRANTA-519, HL-60, THP-1 and Raji cell line, respectively. BI 6727 induced apoptosis, shown by cleaved PARP, in NCI-H460 cells at 100nM post 24h and 48h. An accumulation of mitotic cells with monopolar spindles and positive staining for histone H3 phosphoserine 10 of NCI-H460 cells could also be observed post BI 6727 treatment, confirming that cells are arrested early in the M phase. It exhibited marked antitumor activity in multiple cancer models, including models xenograft HCT 116, NCI-H460 and CXB1 15 cells as well as a model of taxane-resistant colorectal cancer, with oral and i.v. routes of administration at doses ranging in 7-70mg/kg.
作用机制	BI 6727 binds in the ATP binding pocket of Plk1.^[1]

Volasertib 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
5637		Growth Inhibition Assay	48 h	IC50=1165.14 nM	23792639
A431	0-30 nM	Growth Inhibition Assay	1-4 d	inhibits cell growth in both dose- and time-dependent manner	23891096
BRO		Growth Inhibition Assay		EC50 = 11 nM	19383823
DU145	10/50/250 nM	Growth Inhibition Assay	24 h	IC50<10 nM	23884428

Volasertib 动物研究

Dose

Mice: 30 mg/kg^[2] (i.v.), 40 mg/kg^[1] (i.v.), 50 mg/kg^[1] (p.o.) Rat: 10 mg/kg^[1] (i.v.), 30 mg/kg^[1] (p.o.)

Administration

i.v., p.o.

Pharmacokinetics

Animal	Mice^[1]	Rats^[1]
Dose	35 mg/kg (i.v.) 50 mg/kg (p.o.)	10 mg/kg (i.v.) 30 mg/kg (p.o.)
Administration	i.v. p.o.	i.v. p.o.
F	41% (p.o.)	55% (p.o.)
AUC_0→inf	100 µmol·h/l (i.v.)
T_1/2	46 h (i.v.)	54 h (i.v.)
T_max	1.7 h (p.o.)	6.7 h (p.o.)
AUC_0-inf		30 µmol·h/l (i.v.)
CL	10 ml/min/kg (i.v.)	8.9 ml/min/kg (i.v.)
C_max	7.1 µmol/l (i.v.) 5.7 µmol/l (p.o.)	11.9 µmol/l (i.v.) 2.2 µmol/l (p.o.)
Vss	7.6 L/kg (i.v.)	22 L/kg (i.v.)
AUC_0→24h	58 µmol·h/l (p.o.)	34 µmol·h/l (p.o.)

Volasertib 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01023958	Neoplasms	Phase 2	Completed	-	United States, California ... 展开 >> 1230.2.5 Boehringer Ingelheim Investigational Site Beverly Hills, California, United States 1230.2.10 Boehringer Ingelheim Investigational Site Los Angeles, California, United States United States, Florida 1230.2.34 Boehringer Ingelheim Investigational Site Miami, Florida, United States 1230.2.29 Boehringer Ingelheim Investigational Site Orlando, Florida, United States United States, Illinois 1230.2.6 Boehringer Ingelheim Investigational Site Chicago, Illinois, United States 1230.2.17 Boehringer Ingelheim Investigational Site Joliet, Illinois, United States United States, Louisiana 1230.2.24 Boehringer Ingelheim Investigational Site Metairie, Louisiana, United States United States, Maryland 1230.2.1 Boehringer Ingelheim Investigational Site Baltimore, Maryland, United States United States, Nevada 1230.2.25 Boehringer Ingelheim Investigational Site Las Vegas, Nevada, United States 1230.2.36 Boehringer Ingelheim Investigational Site Las Vegas, Nevada, United States United States, New Hampshire 1230.2.19 Boehringer Ingelheim Investigational Site Lebanon, New Hampshire, United States United States, New York 1230.2.20 Boehringer Ingelheim Investigational Site New York, New York, United States 1230.2.23 Boehringer Ingelheim Investigational Site New York, New York, United States United States, North Carolina 1230.2.12 Boehringer Ingelheim Investigational Site Charlotte, North Carolina, United States United States, Pennsylvania 1230.2.4 Boehringer Ingelheim Investigational Site Philadelphia, Pennsylvania, United States United States, Texas 1230.2.38 Boehringer Ingelheim Investigational Site Beaumont, Texas, United States 1230.2.41 Boehringer Ingelheim Investigational Site Tyler, Texas, United States 1230.2.43 Boehringer Ingelheim Investigational Site Webster, Texas, United States United States, Virginia 1230.2.44 Boehringer Ingelheim Investigational Site Fairfax, Virginia, United States Taiwan 1230.2.51 Boehringer Ingelheim Investigational Site Tainan, Taiwan 1230.2.50 Boehringer Ingelheim Investigational Site Taipei, Taiwan 收起 <<
NCT00969553	Neoplasms	Phase 1	Completed	-	Taiwan ... 展开 >> 1230.16.886002 Boehringer Ingelheim Investigational Site Tainan, Taiwan 1230.16.886001 Boehringer Ingelheim Investigational Site Taipei, Taiwan 收起 <<
NCT01023958	-		Completed	-	-

Volasertib 参考文献

[1]Rudolph D, Steegmaier M, et al. BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity. Clin Cancer Res. 2009 May 1;15(9):3094-102.

[2]Gorlick R, Kolb EA, et al. Initial testing (stage 1) of the Polo-like kinase inhibitor volasertib (BI 6727), by the Pediatric Preclinical Testing Program. Pediatr Blood Cancer. 2014 Jan;61(1):158-64.

Volasertib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.62mL

0.32mL

0.16mL

8.08mL

1.62mL

0.81mL

16.16mL

3.23mL

1.62mL

Volasertib 技术信息

CAS号	755038-65-4
分子式	C₃₄H₅₀N₈O₃
分子量	618.81

别名	BI 6727
运输	蓝冰

存储条件

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(80.8 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

4% DMSO+corn oil 2 mg/mL

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01023958	Neoplasms	Phase 2	Completed	-	United States, California ... 展开 >> 1230.2.5 Boehringer Ingelheim Investigational Site Beverly Hills, California, United States 1230.2.10 Boehringer Ingelheim Investigational Site Los Angeles, California, United States United States, Florida 1230.2.34 Boehringer Ingelheim Investigational Site Miami, Florida, United States 1230.2.29 Boehringer Ingelheim Investigational Site Orlando, Florida, United States United States, Illinois 1230.2.6 Boehringer Ingelheim Investigational Site Chicago, Illinois, United States 1230.2.17 Boehringer Ingelheim Investigational Site Joliet, Illinois, United States United States, Louisiana 1230.2.24 Boehringer Ingelheim Investigational Site Metairie, Louisiana, United States United States, Maryland 1230.2.1 Boehringer Ingelheim Investigational Site Baltimore, Maryland, United States United States, Nevada 1230.2.25 Boehringer Ingelheim Investigational Site Las Vegas, Nevada, United States 1230.2.36 Boehringer Ingelheim Investigational Site Las Vegas, Nevada, United States United States, New Hampshire 1230.2.19 Boehringer Ingelheim Investigational Site Lebanon, New Hampshire, United States United States, New York 1230.2.20 Boehringer Ingelheim Investigational Site New York, New York, United States 1230.2.23 Boehringer Ingelheim Investigational Site New York, New York, United States United States, North Carolina 1230.2.12 Boehringer Ingelheim Investigational Site Charlotte, North Carolina, United States United States, Pennsylvania 1230.2.4 Boehringer Ingelheim Investigational Site Philadelphia, Pennsylvania, United States United States, Texas 1230.2.38 Boehringer Ingelheim Investigational Site Beaumont, Texas, United States 1230.2.41 Boehringer Ingelheim Investigational Site Tyler, Texas, United States 1230.2.43 Boehringer Ingelheim Investigational Site Webster, Texas, United States United States, Virginia 1230.2.44 Boehringer Ingelheim Investigational Site Fairfax, Virginia, United States Taiwan 1230.2.51 Boehringer Ingelheim Investigational Site Tainan, Taiwan 1230.2.50 Boehringer Ingelheim Investigational Site Taipei, Taiwan 收起 <<
NCT00969553	Neoplasms	Phase 1	Completed	-	Taiwan ... 展开 >> 1230.16.886002 Boehringer Ingelheim Investigational Site Tainan, Taiwan 1230.16.886001 Boehringer Ingelheim Investigational Site Taipei, Taiwan 收起 <<
NCT01023958	-		Completed	-	-
NCT01121406	Ovarian Neoplasms	Phase 2	Completed	-	Belgium ... 展开 >> 1230.18.32003 Boehringer Ingelheim Investigational Site Brussel, Belgium 1230.18.32004 Boehringer Ingelheim Investigational Site Edegem, Belgium 1230.18.32002 Boehringer Ingelheim Investigational Site Gent, Belgium 1230.18.32001 Boehringer Ingelheim Investigational Site Leuven, Belgium France 1230.18.3321A Boehringer Ingelheim Investigational Site Angers Cedex 9, France 1230.18.3307A Boehringer Ingelheim Investigational Site Bordeaux cedex, France 1230.18.3301A Boehringer Ingelheim Investigational Site Caen, France 1230.18.3322A Boehringer Ingelheim Investigational Site Lille Cedex, France 1230.18.3313A Boehringer Ingelheim Investigational Site Lyon, France 1230.18.3312A Boehringer Ingelheim Investigational Site Nantes cedex 02, France 1230.18.3308A Boehringer Ingelheim Investigational Site Nice cedex, France 1230.18.3314A Boehringer Ingelheim Investigational Site Paris Cedex 20, France 1230.18.3302A Boehringer Ingelheim Investigational Site Paris, France 1230.18.3309A Boehringer Ingelheim Investigational Site Pierre-Bénite cedex, France 1230.18.3305A Boehringer Ingelheim Investigational Site Reims cedex, France 1230.18.3320A Boehringer Ingelheim Investigational Site Saint-Brieuc cedex, France 1230.18.3311A Boehringer Ingelheim Investigational Site Strasbourg, France 1230.18.3310A Boehringer Ingelheim Investigational Site Toulouse Cedex 9, France 1230.18.3315A Boehringer Ingelheim Investigational Site Vandoeuvre les Nancy cedex, France Slovakia 1230.18.42101 Boehringer Ingelheim Investigational Site Bratislava, Slovakia 1230.18.42103 Boehringer Ingelheim Investigational Site Poprad, Slovakia Spain 1230.18.34006 Boehringer Ingelheim Investigational Site Badalona, Spain 1230.18.34001 Boehringer Ingelheim Investigational Site Barcelona, Spain 1230.18.34005 Boehringer Ingelheim Investigational Site Barcelona, Spain 1230.18.34007 Boehringer Ingelheim Investigational Site Girona, Spain 1230.18.34004 Boehringer Ingelheim Investigational Site L'Hospitalet de Llobregat, Spain 1230.18.34002 Boehringer Ingelheim Investigational Site Madrid, Spain 1230.18.34003 Boehringer Ingelheim Investigational Site Madrid, Spain Sweden 1230.18.46005 Boehringer Ingelheim Investigational Site Linköping, Sweden 1230.18.46001 Boehringer Ingelheim Investigational Site Stockholm, Sweden 1230.18.46003 Boehringer Ingelheim Investigational Site Uppsala, Sweden 收起 <<
NCT01121406	-		Completed	-	-
NCT00804856	Leukemia, Myeloid, Acute	Phase 2	Active, not recruiting	August 2, 2019	Austria ... 展开 >> LKH-Univ. Hospital Graz Graz, Austria, 8036 Belgium AZ Sint-Jan Brugge Brugge, Belgium, 8000 Brussels - UNIV Saint-Luc Bruxelles, Belgium, 1200 UZ Leuven Leuven, Belgium, 3000 Canada, Migration Data CHUS Fleurimont Sherbrooke, Migration Data, Canada, J1H 5N4 Canada, Ontario Princess Margaret Cancer Centre Toronto, Ontario, Canada, M5G 2M9 Canada, Quebec Montreal General Hospital - McGill University Health Centre Montreal, Quebec, Canada, H3G 1A4 France HOP Clémenceau, Hémato, Caen Caen, France, 14033 HOP, Centre Hospitalier René Dubos, Hémato, Paris Cergy Pontoise Cedex, France, 95303 HOP Dupuytren Limoges, France, 87042 HOP Herriot Lyon Cedex 03, France, 69437 CTR, fondation Paschetta, Hémato, Nice Nice Cedex 2, France, 06189 HOP Saint-Louis Paris cedex 10, France, 75475 CTR Henri Becquerel Rouen Cedex, France, 76088 Germany Campus Virchow-Klinikum, Berlin Berlin, Germany, 13353 Universitätsklinikum Frankfurt Frankfurt/Main, Germany, 60590 Universitätsklinikum Freiburg Freiburg, Germany, 79106 Universitätsklinikum Hamburg-Eppendorf Hamburg, Germany, 20246 Universitätsklinikum Heidelberg Heidelberg, Germany, 69120 Universitätsklinikum Schleswig-Holstein, Campus Kiel Kiel, Germany, 24116 Universitätsklinikum Münster Münster, Germany, 48149 Universitätsklinikum Ulm Ulm, Germany, 89081 Italy A.O. Spedali Civili di Brescia Brescia, Italy, 25123 ASST Grande Ospedale Metropolitano Niguarda Milano, Italy, 20162 Azienda Ospedaliera Policlinico di Modena Modena, Italy, 41100 Norway Haukeland Universitetssykehus Bergen, Norway, N-5021 Oslo Universitetssykehus HF, Ullevål sykehus Oslo, Norway, N-0450 收起 <<
NCT00824408	Carcinoma, Non-Small-Cell Lung	Phase 2	Completed	-	Bahamas ... 展开 >> 1230.5.00118 Boehringer Ingelheim Investigational Site Nassau, Bahamas Canada, Alberta 1230.5.00104 Boehringer Ingelheim Investigational Site Edmonton, Alberta, Canada Canada, British Columbia 1230.5.00114 Boehringer Ingelheim Investigational Site Kelowna, British Columbia, Canada 1230.5.00109 Boehringer Ingelheim Investigational Site Surrey, British Columbia, Canada 1230.5.00107 Boehringer Ingelheim Investigational Site Vancouver, British Columbia, Canada Canada, Ontario 1230.5.00105 Boehringer Ingelheim Investigational Site Hamilton, Ontario, Canada 1230.5.00119 Boehringer Ingelheim Investigational Site Kitchener, Ontario, Canada 1230.5.00116 Boehringer Ingelheim Investigational Site Oshawa, Ontario, Canada 1230.5.00108 Boehringer Ingelheim Investigational Site Ottawa, Ontario, Canada 1230.5.00110 Boehringer Ingelheim Investigational Site Toronto, Ontario, Canada Canada, Quebec 1230.5.00102 Boehringer Ingelheim Investigational Site Montreal, Quebec, Canada 1230.5.00106 Boehringer Ingelheim Investigational Site Montreal, Quebec, Canada 收起 <<
NCT02273388	Neoplasms	Phase 1	Active, not recruiting	August 26, 2022	Belgium ... 展开 >> 1230.1.32002 Boehringer Ingelheim Investigational Site Brussels, Belgium 1230.1.32001 Boehringer Ingelheim Investigational Site Leuven, Belgium 收起 <<
NCT01721876	Leukemia, Myeloid, Acute	Phase 3	Active, not recruiting	December 31, 2019	-
NCT00824408	-		Completed	-	-
NCT01957644	Myelodysplastic Syndromes ... 展开 >> Leukemia, Myelomonocytic, Chronic 收起 <<	Phase 1	Terminated	-	France ... 展开 >> Boehringer Ingelheim Investigational Site Marseille, France Boehringer Ingelheim Investigational Site Paris, France Germany Boehringer Ingelheim Investigational Site Berlin, Germany Boehringer Ingelheim Investigational Site Dresden, Germany Boehringer Ingelheim Investigational Site Düsseldorf, Germany Boehringer Ingelheim Investigational Site Frankfurt/Main, Germany Boehringer Ingelheim Investigational Site Freiburg, Germany Boehringer Ingelheim Investigational Site Hamburg, Germany Boehringer Ingelheim Investigational Site Hannover, Germany Boehringer Ingelheim Investigational Site Kassel, Germany Boehringer Ingelheim Investigational Site Leipzig, Germany Boehringer Ingelheim Investigational Site Mannheim, Germany Boehringer Ingelheim Investigational Site München, Germany Boehringer Ingelheim Investigational Site Ulm, Germany 收起 <<
NCT01206816	Neoplasms	Phase 1	Completed	-	Belgium ... 展开 >> 1230.20.32001 Boehringer Ingelheim Investigational Site Bruxelles, Belgium 1230.20.32003 Boehringer Ingelheim Investigational Site Edegem, Belgium 1230.20.32002 Boehringer Ingelheim Investigational Site Gent, Belgium 收起 <<
NCT00969761	Neoplasms	Phase 1	Completed	-	Belgium ... 展开 >> 1230.6.3201 Boehringer Ingelheim Investigational Site Bruxelles, Belgium 1230.6.3202 Boehringer Ingelheim Investigational Site Leuven, Belgium 收起 <<
NCT02198482	Acute Myeloid Leukemia (AML) ... 展开 >> High-risk Myelodysplastic Syndrome (MDS) 收起 <<	Phase 2	Terminated(development program... 展开 >> of study drug volasertib was stopped by Boehringer Ingelheim due to manufacturing problems) 收起 <<	-	Germany ... 展开 >> Hospital Aschaffenburg Aschaffenburg, Germany, 63739 Helios Hospital Bad Saarow Bad Saarow, Germany, 15526 Vivantes Hospital Am Urban Berlin, Germany, 10967 Vivantes Hospital Neukölln Berlin, Germany, 12351 Charite Berlin Campus Virchow Hospital Berlin, Germany, 13353 Knappschaftskrankenhaus Bochum-Langendeer Bochum, Germany, 44892 University Hospital Bonn Bonn, Germany, 53105 Community Hospital Braunschweig Braunschweig, Germany, 38114 Hospital Darmstadt Darmstadt, Germany, 64283 University Hospital Düsseldorf Düsseldorf, Germany, 40225 Hospital Essen, Protestant Hospital Essen-Werden Essen, Germany, 45239 Hospital Esslingen Esslingen, Germany, 73730 Malteser Hospital St. Franziskus Flensburg, Germany, 24939 Hospital Frankfurt-Höchst Frankfurt, Germany, 65929 Medical Care Unit Osthessen Fulda, Germany, 36043 University Hospital Gießen Gießen, Germany, 35392 Wilhelm-Anton-Hospital Goch Goch, Germany, 47574 University Hospital Göttingen Göttingen, Germany, 37075 University Hospital Hamburg-Eppendorf Hamburg, Germany, 20246 Asklepios Hospital Altona Hamburg, Germany, 22763 Hospital Hanau Hanau, Germany, 63450 KRH Hospital Siloah-Oststadt-Heidehaus Hannover, Germany, 30459 Hannover Medical School Hannover, Germany, 30625 SLK-Hospital Heilbronn Heilbronn, Germany, 74078 Marienhospital Herne Herne, Germany, 44625 University Hospital des Saarlandes Homburg/Saar, Germany, 66421 Community Hospital Karlsruhe Karlsruhe, Germany, 76133 University Hospital Schleswig-Holstein Kiel, Germany, 24105 Caritas Hospital Lebach Lebach, Germany, 66822 Hospital Lippe-Lemgo Lemgo, Germany, 32657 University Hospital Magdeburg Magdeburg, Germany, 39120 University Hospital Johannes Gutenberg Mainz Mainz, Germany, 55131 Johannes Wesling Hospital Minden Minden, Germany, 32429 Stauferklinikum Schwäbisch-Gmünd Mutlangen, Germany, 73557 Hospital Schwabing München, Germany, 80804 Hospital rechts der Isar München München, Germany, 81675 Hospital Oldenburg Oldenburg, Germany, 26133 Hospital Passau Passau, Germany, 94032 Hospital Stuttgart Stuttgart, Germany, 70174 Diakonie Hospital Stuttgart Stuttgart, Germany, 70176 Hospital Traunstein Traunstein, Germany, 83278 Mutterhaus der Borromäerinnen Trier, Germany, 54290 Hospital Barmherzige Brüder Trier Trier, Germany, 54292 University Hospital Tübingen Tübingen, Germany, 72076 University Hospital Ulm Ulm, Germany, 89081 收起 <<
NCT01022853	-		Completed	-	-
NCT01145885	Neoplasms	Phase 1	Completed	-	Hungary ... 展开 >> 1230.23.36001 Boehringer Ingelheim Investigational Site Budapest, Hungary 收起 <<
NCT01022853	Neoplasms	Phase 1	Completed	-	Italy ... 展开 >> 1230.7.39002 Boehringer Ingelheim Investigational Site Ancona, Italy 1230.7.39001 Boehringer Ingelheim Investigational Site Milano, Italy 收起 <<
NCT01971476	-		Completed	-	-
NCT02875002	Relapsed and Refractory Aggres... 展开 >>sive B- and T-cell Lymphomas Lymphoma 收起 <<	Phase 1	Withdrawn	September 2018	United States, Connecticut ... 展开 >> Yale Cancer Center New Haven, Connecticut, United States, 06511 United States, Maryland Sidney Kimmel Comprehensive Cancer Baltimore, Maryland, United States, 21287 United States, Virginia Massey Cancer Center Richmond, Virginia, United States, 23298 收起 <<
NCT01971476	Leukemia Neop... 展开 >>lasms 收起 <<	Phase 1	Completed	-	Belgium ... 展开 >> UNIV UZ Gent Gent, Belgium, 9000 Czechia University Hospital Motol Prague, Czechia, 150 06 France INS Curie Paris, France, 75248 Germany Universitätsklinikum Köln (AöR) Köln, Germany, 50937 Italy Osp. Pediatrico Bambin Gesù Roma, Italy, 00165 收起 <<
NCT01772563	Neoplasms	Phase 1	Active, not recruiting	April 15, 2019	Hungary ... 展开 >> PRA Hungary Ltd., Phase I. Clinical Pharmacology Unit Budapest, Hungary, 1077 National Institute of Oncology Budapest, Hungary, 1122 收起 <<
NCT02757248	PTCL CTCL	Phase 1	Withdrawn(Boehringer Ingelheim... 展开 >> is discontinuing their volasertib development program) 收起 <<	-	-
NCT02003573	Leukemia, Myeloid, Acute	Phase 1	Terminated	-	United States, Connecticut ... 展开 >> Boehringer Ingelheim Investigational Site New Haven, Connecticut, United States United States, Missouri Boehringer Ingelheim Investigational Site St. Louis, Missouri, United States United States, New York Boehringer Ingelheim Investigational Site Lake Success, New York, United States United States, Texas Boehringer Ingelheim Investigational Site Houston, Texas, United States 收起 <<
NCT01348347	Neoplasms	Phase 1	Completed	-	Japan ... 展开 >> 1230.15.001 National Cancer Center Hospital, Chuo-ku, Tokyo, Japan 收起 <<
NCT02905994	AML	Phase 1	Withdrawn(Funding Withdrawn)	-	United States, Massachusetts ... 展开 >> Massachusetts general Hospital Boston, Massachusetts, United States, 02114 Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02115 收起 <<
NCT01348347	-		Completed	-	-
NCT02527174	Leukemia, Myeloid, Acute ... 展开 >> Leukemia, Monocytic, Acute Leukemia, Myelomonocytic, Acute Leukemia, Erythroblastic, Acute Leukemia, Megakaryoblastic, Acute 收起 <<	Phase 1	Withdrawn(Volasertib no longer... 展开 >> available) 收起 <<	September 2018	Canada, Alberta ... 展开 >> Tom Baker Cancer Centre Calgary, Alberta, Canada, T2N 4N2 University of Alberta Hospital Edmonton, Alberta, Canada, T6G 2G3 收起 <<
NCT02721875	Myelodysplastic Syndromes	Phase 1	Terminated	-	Japan ... 展开 >> University of Fukui Hospital Fukui, Yoshida-gun, Japan, 910-1193 收起 <<
NCT02861040	Recurrent Adult Acute Lymphobl... 展开 >>astic Leukemia Refractory Adult Acute Lymphoblastic Leukemia 收起 <<	Phase 1	Withdrawn	-	United States, California ... 展开 >> Stanford University Palo Alto, California, United States, 94304 United States, Maryland Johns Hopkins University/Sidney Kimmel Cancer Center Baltimore, Maryland, United States, 21231 收起 <<
NCT02721875	-		Terminated	-	-
NCT02201329	Myelodysplastic Syndromes ... 展开 >> Leukemia, Myelomonocytic, Chronic 收起 <<	Phase 1	Completed	-	Japan ... 展开 >> Boehringer Ingelheim Investigational Site Aichi, Nagoya, Japan Boehringer Ingelheim Investigational Site Gunma, Maebashi, Japan Boehringer Ingelheim Investigational Site Nagasaki, Nagasaki, Japan Boehringer Ingelheim Investigational Site Tokyo, Sinagawa-ku, Japan 收起 <<
NCT02201329	-		Completed	-	-
NCT02722135	Leukemia, Myeloid, Acute	Phase 1	Withdrawn	September 2018	Belgium ... 展开 >> Boehringer Ingelheim Investigational Site Gent, Belgium 收起 <<
NCT01662505	Leukemia, Myeloid, Acute	Phase 1	Completed	-	Japan ... 展开 >> Boehringer Ingelheim Investigational Site Chuo-ku, Tokyo, Japan Boehringer Ingelheim Investigational Site Isehara, Kanagawa, Japan Boehringer Ingelheim Investigational Site Maebashi, Gunma,, Japan Boehringer Ingelheim Investigational Site Nagasaki, Nagasaki, Japan Boehringer Ingelheim Investigational Site Nagoya-shi, Aichi, Japan Boehringer Ingelheim Investigational Site Yoshida-gun, Fukui, Japan 收起 <<
NCT01662505	-		Completed	-	-

5637		Growth Inhibition Assay	48 h	IC50=1165.14 nM	23792639
A431	0-30 nM	Growth Inhibition Assay	1-4 d	inhibits cell growth in both dose- and time-dependent manner	23891096
BRO		Growth Inhibition Assay		EC50 = 11 nM	19383823
DU145	10/50/250 nM	Growth Inhibition Assay	24 h	IC50<10 nM	23884428
FaDu	0-1000 nM	Growth Inhibition Assay	1-4 d	inhibits cell growth in both dose- and time-dependent manner	23891096
GRANTA-519		Growth Inhibition Assay		EC50 = 15 nM	19383823
HCC1428/LTED	2.5-40 nM	Growth Inhibition Assay	5 d	inhibits cell growth in a dose-dependent manner	25480943
HCT 116		Growth Inhibition Assay		EC50 = 23 nM	19383823
HL-60		Growth Inhibition Assay		EC50 = 32 nM	19383823
HUCCT-1	200 nM	Apoptosis Assay	24 h	induces apoptosis	23703673
KASUMI-1		Growth Inhibition Assay	72 h	IC50=170±51 nM	25576074
KG-1		Growth Inhibition Assay	72 h	IC50=150±67 nM	25576074
KMCH-1	200 nM	Apoptosis Assay	24 h	induces apoptosis	23703673
LNCaP	10/50/250 nM	Growth Inhibition Assay	24 h	IC50<10 nM	23884428
MCF7/LTED	2.5-40 nM	Growth Inhibition Assay	5 d	inhibits cell growth in a dose-dependent manner	25480943
MOLM-13		Growth Inhibition Assay	72 h	IC50=57±44 nM	25576074
MV-4-11		Growth Inhibition Assay	72 h	IC50=16±6 nM	25576074
Mz-ChA-1	200 nM	Apoptosis Assay	24 h	induces apoptosis	23703673
NCI-H460		Growth Inhibition Assay		EC50 = 21 nM	19383823
NOMO-1		Growth Inhibition Assay	72 h	IC50=145±7 nM	25576074
OCI-AML3		Growth Inhibition Assay	72 h	IC50=90±51 nM	25576074
PC3	10/50/250 nM	Growth Inhibition Assay	24 h	IC50∼600 nM	23884428
Raji		Growth Inhibition Assay		EC50 = 37 nM	19383823
RT4		Growth Inhibition Assay	48 h	IC50=111.27 nM	23792639
SF188	50-150 nM	Growth Inhibition Assay	72 h	inhibits cell proliferation	23887645
SKM-1		Growth Inhibition Assay	72 h	IC50=95±52 nM	25576074
T24		Growth Inhibition Assay	48 h	IC50=204.91 nM	23792639
T98G	50-150 nM	Growth Inhibition Assay	72 h	inhibits cell proliferation	23887645
THP-1		Growth Inhibition Assay	72 h	IC50=56±39 nM	25576074
THP-1		Growth Inhibition Assay		EC50 = 36 nM	19383823

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