Chemical Property of Volasertib
Chemical Property:
- PKA:14.26±0.40(Predicted)
- PSA：106.17000
- Density:1.26
- LogP:4.73690
- Storage Temp.:-20°
- Solubility.:Soluble in DMSO (up to at least 25 mg/ml).
- XLogP3:4.6
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:9
- Rotatable Bond Count:10
- Exact Mass:618.40058749
- Heavy Atom Count:45
- Complexity:996
- Purity/Quality:
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99%, *data from raw suppliers
Volasertib *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CCC1C(=O)N(C2=CN=C(N=C2N1C(C)C)NC3=C(C=C(C=C3)C(=O)NC4CCC(CC4)N5CCN(CC5)CC6CC6)OC)C
- Isomeric 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
- Recent ClinicalTrials:Volasertib in Combination With Low-dose Cytarabine in Patients Aged 65 Years and Above With Previously Untreated Acute Myeloid Leukaemia, Who Are Ineligible for Intensive Remission Induction Therapy (POLO-AML-2)
- Recent EU Clinical Trials:Open-label, dose-escalating trial to evaluate the tolerability, toxicity, safety, pharmacokinetics, pharmacodynamics and activity of volasertib added to the standard intensive salvage chemotherapy regimen with liposomal daunorubicine, fludarabine and cytarabine (DNX-FLA) followed by fludarabine and cytarabine (FLA) in children from 3 months to less than 18 years of age with acute myeloid leukaemia after failure of the front-line therapy
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Description
Volasertib (BI 6727) is a highly potent Plk1 inhibitor with IC50 of 0.87 nM in a cell-free assay. It shows 6-and 65-fold greater selectivity against Plk2 and Plk3. Phase 3. 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).
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Uses
Volasertib (BI 6727) is a highly potent Polo-like kinase (PLK) inhibitor.
