(S)-2-(1-((2-aMino-9H-purin-6-yl)aMino)ethyl)-5-Methyl-3-(o-tolyl)quinazolin-4(3H)-one hydrochloride

(S)-2-(1-((2-aMino-9H-purin-6-yl)aMino)ethyl)-5-Methyl-3-(o-tolyl)quinazolin-4(3H)-one hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  CAL-130 Hydrochloride is a PI3Kδ and PI3Kγ inhibitor with IC50 of 1.3 and 6.1 nM, respectively.

• in vitro

  CAL-130 preferentially inhibits the function of both p110γ and p110δ catalytic domains. IC ₅₀ values of CAL-130 are 1.3 and 6.1 nM for p110δ and p110γ, respectively, as compared to 115 and 56 nM for p110α and p110β. CAL-130 does not inhibit additional intracellular signaling pathways (ie, p38 MAPK or insulin receptor tyrosine kinase) that are critical for general cell function and survival.

• in vivo

  The clinical significance of interfering with the combined activities of PI3Kγ and PI3Kδ is determined by administering CAL-130 to Lck/Pten ^fl/fl mice with established T cell acute lymphoblastic leukemia (T-ALL). Candidate animals for survival studies are ill appearing, have a white blood cell (WBC) count above 45,000 μL ^-1 , evidence of blasts on peripheral smear, and a majority of circulation cells (>75%) staining double positive for Thy1.2 and Ki-67. Mice receive an oral dose (10 mg/kg) of CAL-130 every 8 hr for a period of 7 days and are then followed until moribund. Despite the limited duration of therapy, CAL-130 is highly effective in extending the median survival for treated animals to 45 days as compared 7.5 days for the control group.

• target

  PI3K

(S)-2-(1-((2-aMino-9H-purin-6-yl)aMino)ethyl)-5-Methyl-3-(o-tolyl)quinazolin-4(3H)-one hydrochloride Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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