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ChemicalBook--->CAS DataBase List--->1431697-78-7

1431697-78-7

1431697-78-7 Structure

1431697-78-7 Structure
IdentificationBack 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
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

Soluble in DMSO
[form ]

Powder
[color ]

Light yellow to yellow
Hazard InformationBack 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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