Chemical Structure : PLK1 inhibitor B9
CAS No.:
3067303-49-2
PLK1 inhibitor B9
Catalog No.: PC-27199Not For Human Use, Lab Use Only.
PLK1 inhibitor B9 is a potent, selective, covalent inhibitor of polo-like kinase 1 (PLK1) with IC50 of 19 nM, shows exceptional cellular potency with IC50 of 0.4 nM in K562 leukemia cells.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
PLK1 inhibitor B9 is a potent, selective, covalent inhibitor of polo-like kinase 1 (PLK1) with IC50 of 19 nM, shows exceptional cellular potency with IC50 of 0.4 nM in K562 leukemia cells.
B9 shows >150-fold improvement over the reversible reference compound BI2536 (K562 cell IC50=61 nM).
K562 shows favorable overall selectivity against nonrelated kinases.
B9 (10-20 mg/kg, i.p.) significantly suppressed the bioluminescence of leukemia burden and extended survival rates to 100% over 42 days without observable toxicity.
Physicochemical Properties
|
M.Wt
|
551.62
|
|
Formula
|
C28H34FN7O4
|
|
Appearance
|
Solid
|
|
CAS No.
|
|
|
Storage
|
- Solide Powder
-
-20°C 12 Months; 4°C 6 Months
|
- In Solvent
-
-80°C 6 Months; -20°C 6 Months
|
|
Shipping
|
|
|
Solubility
|
10 mM in DMSO
|
|
Chemical Name/SMILES
|
(R)-4-((8-(1-acryloylpiperidin-4-yl)-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl)amino)-N-cyclopropyl-2-fluoro-5-methoxybenzamide
|
References
1. Zhou J, et al. J Med Chem. 2026 Jun 30. doi: 10.1021/acs.jmedchem.6c01512.
Contact Us
sales@probechem.com
