| Identification | Back 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 |
| Hazard Information | Back 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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| Company Name: |
LETOPHARM LIMITED
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| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
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