XL413 (BMS-863233) Chemical Properties

storage temp. 

-20°C

solubility 

DMSO: Insoluble;Ethanol: Insoluble

form 

powder

color 

white to beige

Water Solubility 

Water: 46 mg/mL (141.03 mM)

Stability:

Hygroscopic

Safety Information

RIDADR 

UN 2811 6.1 / PGIII

XL413 (BMS-863233) Usage And Synthesis

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

< td class="border-bottom: 1px dotted #ccc;padding: 5px;"> CK2
(Cell-free assay)

Target	Value
Cdc7 (Cell-free assay)	3.4 nM
Pim1 (Cell-free assay)	42 nM
212 nM

storage

Store at -20°C

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