Uses
XL413 is a potent and selective cell division cycle 7 homolog (CDC7) kinase inhibitor.
Biological Activity
XL413 hydrochloride is a potent and selective cell division cycle 7 homolog (CDC7) kinase inhibitor with IC50 of 3.4 nM, its selectivity over CK2, Pim-1 and pMCM2 are 63-, 12- and 35-fold. Phase 1/2.
in vitro
In MDA-MB-231T and Colo-205 cell lines,XL413 hydrochloride inhibits CDC7-specific phosphorylation of MCM2. XL413 also inhibited cell proliferation in Colo-205 cells, decreased cell viability, and stimulated caspase 3/7 activity. Furthermore, XL413 resulted in altered S-phase progression and subsequent apoptosis.
in vivo
In the Colo-205 xenograft model, XL413, at a dose of 3 mg/kg, inhibited 70% of phosphorylated MCM2 and caused significant regression of tumor growth at a dose of 100 mg/kg.
target
| Target | Value |
Cdc7
(Cell-free assay) | 3.4 nM |
Pim1
(Cell-free assay) | 42 nM |
< td style="border-bottom: 1px dotted #ccc;padding: 5px;"> CK2
(Cell-free assay) 212 nM |
