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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Volasertib (formerly also known as BI6727, BI-6727, BI 6727) is a novel and highly potent dihydropteridinone-based Plk1 (polo-like kinase 1) inhibitor with potential antineoplastic activity. In a test without cells, it inhibits Plk1 with an IC50 of 0.87 nM. Comparing volasertib to Plk2 and Plk3, the drug exhibits 6- and 65-fold higher selectivity. BI 6727 selectively inhibits Plk1, causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells, and selective G2/M arrest followed by apoptosis in a variety of tumor cells. With unique properties, BI 6727 is a highly potent and selective dihydropteridinone (enzyme IC50 = 0.87 nmol/L, EC50 = 11-37 nmol/L on a panel of cancer cell lines).
Targets |
PLK1 (IC50 = 0.87 nM); PLK2 (IC50 = 5 nM); PLK3 (IC50 = 56 nM)
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
Human Plk1 recombinant (residues 1–603) is purified by affinity chromatography employing glutathione-agarose after being expressed as an NH2-terminal, GST-tagged fusion protein using a baculoviral expression system. Using 10 μg of bovine milk casein as the substrate and 20 ng of recombinant kinase, Plk1 enzyme activity assays are conducted in the presence of serially diluted BI6727. 15 mM MgCl2, 25 mM MOPS (pH 7.0), 1 mM DTT, 1% DMSO, 7.5 μM ATP, and 0.3 μCi γ-32P-ATP are the ingredients for kinase reactions, which are carried out in a final volume of 60 μL for 45 minutes at 30 °C. When 125 μL of ice-cold 5% TCA is added, the reaction is stopped. Radiometric quantification is performed on MultiScreen mixed ester cellulose filter plates following the transfer of precipitates, followed by a 1% TCA wash. The IC50 value is computed using dose-response curves.
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Cell Assay |
In assays for cell proliferation, different concentrations of BI6727 are added to cells and incubated for 24, 48, and 72 hours. The growth of the cells is evaluated by measuring the conversion of Alamar blue dye in a fluorescence spectrophotometer. From the dose-response curve fit, effective concentrations (EC50) at which cellular growth is inhibited by 50% are extrapolated. Cell suspensions are fixed in 80% ethanol, treated with 0.25% Triton X-100 in PBS for 5 minutes, and then incubated for 20 minutes at room temperature with 0.1% RNase and 10 μg/mL propidium iodide in PBS. Flow cytometric analysis is used to determine cell cycle profiles.
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Animal Protocol |
Female BomTac:NMRI-Foxn1nu mice grafted s.c. with HCT116, NCI-H460, or CXB1 cells
~25 mg/kg/day Injected i.v., or given intragastrally via gavage needle |
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References |
Molecular Formula |
C34H50N8O3
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Molecular Weight |
618.81
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Exact Mass |
618.40
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Elemental Analysis |
C, 65.99; H, 8.14; N, 18.11; O, 7.76
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CAS # |
755038-65-4
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Appearance |
White to off-white solid powder
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SMILES |
CC[C@@H]1C(=O)N(C2=CN=C(N=C2N1C(C)C)NC3=C(C=C(C=C3)C(=O)NC4CCC(CC4)N5CCN(CC5)CC6CC6)OC)C
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InChi Key |
SXNJFOWDRLKDSF-XKHVUIRMSA-N
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InChi Code |
InChI=1S/C34H50N8O3/c1-6-28-33(44)39(4)29-20-35-34(38-31(29)42(28)22(2)3)37-27-14-9-24(19-30(27)45-5)32(43)36-25-10-12-26(13-11-25)41-17-15-40(16-18-41)21-23-7-8-23/h9,14,19-20,22-23,25-26,28H,6-8,10-13,15-18,21H2,1-5H3,(H,36,43)(H,35,37,38)/t25?,26?,28-/m1/s1
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Chemical Name |
N-[4-[4-(cyclopropylmethyl)piperazin-1-yl]cyclohexyl]-4-[[(7R)-7-ethyl-5-methyl-6-oxo-8-propan-2-yl-7H-pteridin-2-yl]amino]-3-methoxybenzamide
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Synonyms |
BI6727; BI 6727; BI-6727; Volasertib
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6160 mL | 8.0800 mL | 16.1600 mL | |
5 mM | 0.3232 mL | 1.6160 mL | 3.2320 mL | |
10 mM | 0.1616 mL | 0.8080 mL | 1.6160 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT01772563 | Completed | Drug: volasertib Drug: itraconazole |
Neoplasms | Boehringer Ingelheim | February 4, 2013 | Phase 1 |
NCT01662505 | Completed | Drug: Volasertib | Leukemia, Myeloid, Acute | Boehringer Ingelheim | August 2012 | Phase 1 |
NCT02201329 | Completed | Drug: Azacitidine Drug: Volasertib |
Myelodysplastic Syndromes Leukemia, Myelomonocytic, Chronic |
Boehringer Ingelheim | August 2014 | Phase 1 |
NCT00969553 | Completed | Drug: BI 6727 | Neoplasms | Boehringer Ingelheim | August 2009 | Phase 1 |
NCT01145885 | Completed | Drug: BI 6727 | Neoplasms | Boehringer Ingelheim | June 2010 | Phase 1 |
Volasertib inhibits the growth of cervical cancer cellsin vitro.Am J Cancer Res.2015 Nov 15;5(12):3548-59. th> |
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Volasertib induces cell cycle arrest at G2/M Phase in cervical cancer cells.Am J Cancer Res.2015 Nov 15;5(12):3548-59. td> |
Volasertib induces apoptosis in cervical cancer cells.Am J Cancer Res.2015 Nov 15;5(12):3548-59. td> |
Volasertib induces ROS accumulation in cervical cancer cells. Volasertib potentiates the activity of cisplatin to inhibit the growth of cervical cancer cellsin vitro.Am J Cancer Res.2015 Nov 15;5(12):3548-59. th> |
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Inhibition of ROS partially rescues volasertib-induces apoptosis in cervical cancer cells.Am J Cancer Res.2015 Nov 15;5(12):3548-59. td> |
Volasertib potentiates the activity of cisplatin to inhibit xenograft tumor growth of cervical cancer cells in nude mice.Am J Cancer Res.2015 Nov 15;5(12):3548-59. td> |