Volasertib | Potent and selective inhibitor of Polo-like kinase 1
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $80.00 | ||
| 25 mg | $275.00 |
Volasertib (755038-65-4) is an extremely potent and selective inhibitor (IC50’s: Plk1= 0.87 nM, Plk2 = 5 nM, Plk3 = 56 nM) of Polo-like kinase 1, a critical controller of multiple essential steps of mitosis.1 It has shown efficacy in multiple solid xenograft tumors models1 and in clinical studies in patients with acute myeloid leukemia2. Volasertib has also been shown to potently inhibit BRD43 (Kd = 79 nM3, IC50’s bromodomains 1 and 2 of BRD4 = 300 and 770 nM respectively2).
References/Citations:
1) Rudolph et al. (2009) BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity; Clin. Cancer Res. 15 3094
2) Rudolph et al. (2015) Efficacy and Mechanism of Action of Volasertib, a Potent and Selective Inhibitor of Polo-Like Kinases, in Preclinical Models of Acute Myeloid Leukemia; J. Pharmacol. Exp. Ther. 352 579
3) Ciceri et al. (2014) Dual kinase-bromodomain inhibitors for rationally designed polypharmacology; Nat. Chem. Biol. 10 305
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
Volasertib (755038-65-4) is an extremely potent and selective inhibitor (IC50’s: Plk1= 0.87 nM, Plk2 = 5 nM, Plk3 = 56 nM) of Polo-like kinase 1, a critical controller of multiple essential steps of mitosis.1 It has shown efficacy in multiple solid xenograft tumors models1 and in clinical studies in patients with acute myeloid leukemia2. Volasertib has also been shown to potently inhibit BRD43 (Kd = 79 nM3, IC50’s bromodomains 1 and 2 of BRD4 = 300 and 770 nM respectively2).
References/Citations:
1) Rudolph et al. (2009) BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity; Clin. Cancer Res. 15 3094
2) Rudolph et al. (2015) Efficacy and Mechanism of Action of Volasertib, a Potent and Selective Inhibitor of Polo-Like Kinases, in Preclinical Models of Acute Myeloid Leukemia; J. Pharmacol. Exp. Ther. 352 579
3) Ciceri et al. (2014) Dual kinase-bromodomain inhibitors for rationally designed polypharmacology; Nat. Chem. Biol. 10 305
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Focus Biomolecules • Plymouth Meeting, PA USA • 1-855-FOCUS21
Focus Biomolecules
Plymouth Meeting, PA USA
1-855-FOCUS21
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