Identification | Back Directory | [Name]
(S)-2-(1-((2-aMino-9H-purin-6-yl)aMino)ethyl)-5-Methyl-3-(o-tolyl)quinazolin-4(3H)-one hydrochloride | [CAS]
1431697-78-7 | [Synonyms]
CAL-130 HCl CAL-130 (Hydrochloride) (S)-2-(1-((2-aMino-9H-purin-6-yl)aMino)ethyl)-5-Methyl-3-(o-tolyl)quinazolin-4(3H)-one hydrochloride 2-[(1S)-1-[(2-Amino-9H-purin-6-yl)amino]ethyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone hydrochloride (1:1) | [Molecular Formula]
C23H23ClN8O | [MDL Number]
MFCD25372043 | [MOL File]
1431697-78-7.mol | [Molecular Weight]
462.935 |
Hazard Information | Back Directory | [Biological Activity]
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 |
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Company Name: |
Musechem
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Tel: |
+1-800-259-7612 |
Website: |
www.musechem.com |
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