Volasertib (BI 6727)
- CAS NO.:755038-65-4
- Empirical Formula: C34H50N8O3
- Molecular Weight: 618.81
- MDL number: MFCD20926414
- EINECS: 813-258-1
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-08 09:02:25
What is Volasertib (BI 6727)?
Description
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).
The Uses of Volasertib (BI 6727)
Volasertib (BI 6727) is a highly potent Polo-like kinase (PLK) inhibitor.
What are the applications of Application
BI6727 is an ATP-competitive Plk1/2/3 inhibitor
References
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
Properties of Volasertib (BI 6727)
Melting point: | 86 - 87*C |
Density | 1.26 |
storage temp. | -20° |
solubility | Soluble in DMSO (up to at least 25 mg/ml). |
form | solid |
pka | 14.26±0.40(Predicted) |
color | Off-white |
Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
CAS DataBase Reference | 755038-65-4 |
Safety information for Volasertib (BI 6727)
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation |
Precautionary Statement Codes |
P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. P332+P313:IF SKIN irritation occurs: Get medical advice/attention. P337+P313:IF eye irritation persists: Get medical advice/attention. |
Computed Descriptors for Volasertib (BI 6727)
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