XL413 (BMS-863233)

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Achtung

• Gefahrenhinweise

  H301：Giftig bei Verschlucken.

XL413 (BMS-863233) Chemische Eigenschaften,Einsatz,Produktion Methoden

• Verwenden

  XL413 is a potent and selective cell division cycle 7 homolog (CDC7) kinase inhibitor.

• Biologische Aktivität

  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 style="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

• Lager

  Store at -20°C

XL413 (BMS-863233) Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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