|
| | XL413 (BMS-863233) Basic information |
| Product Name: | XL413 (BMS-863233) | | Synonyms: | 8-Chloro-2-(2S)-2-pyrrolidinylbenzofuro[3,2-d]pyrimidin-4(3H)-one hydrochloride;CS-1062;XL 413 hydrochloride - BMS 863233 hydrochloride;BMS-863233; BMS863233; BMS 863233; XL-413; XL413; XL 413.;Benzofuro[3,2-d]pyriMidin-4(3H)-one, 8-chloro-2-(2S)-2-pyrrolidinyl-, (Hydrochloride) (1:);XL413 (hydrochloride);BMS-863233 (XL-413);8-Chloro-2-(2S)-2-pyrrolidinylbenzofuro[3,2-d]pyrimidin-4(3H)-one hydrochloride (1:?) | | CAS: | 1169562-71-3 | | MF: | C14H13Cl2N3O2 | | MW: | 326.18 | | EINECS: | | | Product Categories: | Inhibitors;API | | Mol File: | 1169562-71-3.mol |  |
| | 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 |
| 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 | | 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 |
|
