Volasertib | Potent and selective inhibitor of Polo-like kinase 1

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

Weight 0.01 mg
Dimensions 0.01 × 0.01 × 0.01 cm
Size:

5 mg, 25 mg

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CAS:
755038-65-4
Catalog Number:
10-4818
Activity:
Potent and selective inhibitor of Polo-like kinase 1
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
Alternate Name:
BI 6727
Molecular Weight:
618.82
Molecular Formula:
C34H50N8O3
Solubility:
Soluble in DMSO (up to at least 25 mg/ml).
Physical Properties:
Off-white solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT

Volasertib | Potent and selective inhibitor of Polo-like kinase 1

$80.00$275.00

CAS:
755038-65-4
Catalog Number:
10-4818
Activity:
Potent and selective inhibitor of Polo-like kinase 1
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
Alternate Name:
BI 6727
Molecular Weight:
618.82
Molecular Formula:
C34H50N8O3
Solubility:
Soluble in DMSO (up to at least 25 mg/ml).
Physical Properties:
Off-white solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT
  • 5 mg
  • 25 mg
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