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Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,520 | 6-8 weeks | |
50 mg | $1,980 | 6-8 weeks | |
100 mg | $2,500 | 6-8 weeks |
Description | CAL-130 is a PI3Kδ and PI3Kγ inhibitor (IC50s: 1.3 and 6.1 nM). |
In vitro | CAL-130 preferentially inhibits the function of both p110γ and p110δ catalytic domains (IC50s: 1.3 and 6.1 nM for p110δ and p110γ, 115 and 56 nM for p110α and p110β). CAL-130 does not inhibit additional intracellular signaling pathways (i.e., p38 MAPK or insulin receptor tyrosine kinase) that are critical for general cell function and survival. |
In vivo | The clinical impact of inhibiting both PI3Kγ and PI3Kδ activities is assessed through the administration of CAL-130 to Lck/Pten^fl/fl mice suffering from established T cell acute lymphoblastic leukemia. Selection of mice for the survival study is based on criteria including poor health appearance, a white blood cell count exceeding 45,000/μL, presence of blast cells in peripheral blood smear, and over 75% of circulating cells being double-positive for Thy1.2 and Ki-67 markers. These mice are then treated with an oral dosage (10 mg/kg) of CAL-130 every eight hours for a week, and their health outcomes are monitored until they become moribund. Despite the short treatment period, CAL-130 significantly increases the median survival rate of these mice to 45 days, in stark contrast to the 7.5 days survival of the control group. |
Molecular Weight | 426.47 |
Formula | C23H22N8O |
Cas No. | 1431697-74-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
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