Research Area
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BI6727 (Volasertib) Chemical Structure
BI 2536
BI 2536 is a Plk1 inhibitor with an IC50 of 0.83 nM.
TAK-960
TAK-960 is a novel, potent and selective PLK1 inhibitor with a minimal IC50 of 8 nM.
ON-01910
ON-01910 (Estybon, Novonex, Rigosertib) is a non-ATP-competitive inhibitor to Polo-like kinase 1 (PLK1) with IC50 of 9 nM.
HMN-214
HMN-214 is a potent PLK1 inhibitor an average IC50 of 0.12 μM.
ABT-888 (Veliparib)
ABT-888 (Veliparib) is a potent poly (ADP-ribose) polymerase (PARP) inhibitor of PARP-1 and PARP-2 with Ki of 5.2 nM and 2.9 nM, respectively.
Olaparib (AZD2281)
Olaparib(AZD2281, KU0059436) is a selective inhibitor of PARP-1 and PARP-2 enzymes with IC50 of 5 nM and 1 nM, respectively.
Y-27632 2HCl
Y-27632 2HCl is ROCK inhibitor, as a novel bronchodilator. Y27632 is available with IC50 of 3.3±0.25 μM and 2.8±0.2 μM in human and rabbit tissues, respectively.
Rucaparib (AG-014699 , PF-01367338)
AG-014699 (Rucaparib, PF-01367338) is an inhibitor of PARP with a Ki of 1.4 nM.
BI 2536
BI 2536 is a Plk1 inhibitor with an IC50 of 0.83 nM.
Biological Activity
BI 6727 is a highly potent Polo-like kinase inhibitor with an IC50 of 0 .87 nM BI 6727 has an EC50 of 11-37 nM on a panel of cancer cell lines and selective dihydropteridinone with distinct properties. BI 6727 has a pharmacokinetic profile favoring sustained exposure of tumor tissues with a high volume of distribution and a long terminal half-life in mice. BI 6727 has physicochemical and pharmacokinetic properties that allow in vivo testing of i.v. as well as oral formulations, adding flexibility to dosing schedules. BI 6727 shows marked antitumor activity in multiple cancer models, including a model of taxane-resistant colorectal cancer. [1][2][3]
References on BI6727 (Volasertib)
- [1] Clin Cancer Res 2009;15:3094-3102
- [2] The Oncologist 2009;14:559–570
- [3] Cancer Res 2011;71:1385-1395
Product Information
| Molecular Weight (WM): | 618.81 |
|---|---|
| Formula: | C34H50N8O3 |
| CAS No.: | 755038-65-4 |
| Synonyms: |
Volasertib
|
| Dissolve in (25°C): | DMSO ≥23mg/mL |
| Water <1mg/mL | |
| Ethanol ≥124mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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Decrease viability of Hec50 subclones after 3 days treatment with BI6727 was shown. Reduction of Cdc2 Tyr15 phosphorylation and increase Histone H3 Ser10 phosphorylation in cells treated with BI 6727 was observed.
Decrease viability of Hec50 subclones after 3 days treatment with BI6727 was shown. Reduction of Cdc2 Tyr15 phosphorylation and increase Histone H3 Ser10 phosphorylation in cells treated with BI 6727 was observed.
Data independently produced by Dr Xiangbing Meng from University of Iowa BI6727 (Volasertib) purchased from Selleck
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Click to enlarge
Hec50 cells are arrested in mitosis after 24hours treatment with 10nM BI 6727.
Hec50 cells are arrested in mitosis after 24hours treatment with 10nM BI 6727.
Data independently produced by Dr Xiangbing Meng from University of Iowa BI6727 (Volasertib) purchased from Selleck
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Decrease viability of Hec50 subclones after 3 days treatment with BI6727 was shown. Reduction of Cdc2 Tyr15 phosphorylation and increase Histone H3 Ser10 phosphorylation in cells treated with BI 6727 was observed. |
Data independently produced by Dr Xiangbing Meng from University of Iowa
Hec50 cells are arrested in mitosis after 24hours treatment with 10nM BI 6727. |
Data independently produced by Dr Xiangbing Meng from University of Iowa
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