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ChemicalBook--->CAS DataBase List--->1431697-74-3

1431697-74-3

1431697-74-3 Structure

1431697-74-3 Structure
IdentificationBack Directory
[Name]

CAL 130
[CAS]

1431697-74-3
[Synonyms]

CAL130; CAL 130
4(3H)-Quinazolinone, 2-[(1S)-1-[(2-amino-9H-purin-6-yl)amino]ethyl]-5-methyl-3-(2-methylphenyl)-
[Molecular Formula]

C23H22N8O
[MDL Number]

MFCD25372030
[MOL File]

1431697-74-3.mol
[Molecular Weight]

426.47
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

DMSO
[form ]

Powder
Hazard InformationBack Directory
[Uses]

CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC50s of 1.3 and 6.1 nM, respectively.
[in vivo]

The clinical significance of interfering with the combined activities of PI3Kγ and PI3Kδ is determined by administering CAL-130 to Lck/Ptenfl/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[1].

[IC 50]

p110δ: 1.3 nM (IC50); p110γ: 6.1 nM (IC50); p110β: 56 nM (IC50); p110α: 115 nM (IC50)
[storage]

Store at -20°C
[References]

[1] Subramaniam Prem S, et al. Targeting nonclassical oncogenes for therapy in T-ALL. Cancer cell (2012), 21(4), 459-72. DOI:10.1016/j.ccr.2012.02.029
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