CX-4945, CK2 (Casein Kinase 2) Inhibitor

Overview
Catalog #	bs-60267c-2-mg-solid
Product Name	CX-4945, CK2 (Casein Kinase 2) Inhibitor
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 349.77 Formula: C19 H12 Cl N3 O2 CAS Number: 1009820-21-6 InChi Key: MUOKSQABCJCOPU-UHFFFAOYSA-N InChi: InChI=1S/C19H12ClN3O2/c20-12-2-1-3-13(9-12)22-18-15-6-7-21-10-16(15)14-5-4-11(19(24)25)8-17(14)23-18/h1-10H,(H,22,23)(H,24,25) Smiles: OC(=O)C1=CC2N=C(NC3=CC(Cl)=CC=C3)C3=CC=NC=C3C=2C=C1 Purity: 98.0 Solubility: DMSO up to 40 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	CX-4945 (Silmitasertib) is a potent, selective and bioavailable CK2 (Casein Kinase 2) Inhibitor with IC50 of 1 nM. It only inhibits 7 of the 238 kinases by more than 90% at concentration of 0.5 μM, which is 500-fold selectivity over CK2. Although in cell-free systems CX-4945 inhibits FLT3, PIM1, and CDK1 with IC50 of 35 nM, 46 nM, and 56 nM, respectively, but it is inactive against FLT3, PIM1, and CDK1 in cell-based functional assays at 10 µM. CX-4945 exhibits a broad spectrum of antiproliferative activity, correlates with CK2α mRNA and protein levels but not the CK2α' catalytic subunit, the regulatory CK2β subunit, and the PI3K/Akt or PTEN mutational status. Combined inhibition of EGFR and CK2 augments the attenuation of PI3K-Akt-mTOR signaling and the killing of cancer cells. CX-4945 can potentiate senescence by blocking tumour progression in Ptenpc -/- mice. Now CX-4945 is in phase I/II clinical trials to treat cancer.