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CAL-130

Catalog No. T10660Cas No. 1431697-74-3

CAL-130 is a PI3Kδ and PI3Kγ inhibitor [IC50s: 1.3 and 6.1 nM].

CAL-130

CAL-130

Catalog No. T10660Cas No. 1431697-74-3
CAL-130 is a PI3Kδ and PI3Kγ inhibitor [IC50s: 1.3 and 6.1 nM].
Pack SizePriceAvailabilityQuantity
25 mg$1,5206-8 weeks
50 mg$1,9806-8 weeks
100 mg$2,5006-8 weeks
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Product Introduction

Bioactivity
Description
CAL-130 is a PI3Kδ and PI3Kγ inhibitor [IC50s: 1.3 and 6.1 nM].
Targets&IC50
p110δ:1.3 nM, p110γ:6.1 nM, p110α:115 nM, p110β:56 nM
In vitro
CAL-130 selectively inhibits the catalytic domains of p110γ and p110δ (IC50s: 1.3 and 6.1 nM for p110δ and p110γ, 115 and 56 nM for p110α and p110β) without affecting other intracellular signaling pathways such as p38 MAPK or insulin receptor tyrosine kinase, which are essential for overall 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.
Chemical Properties
Molecular Weight426.47
FormulaC23H22N8O
Cas No.1431697-74-3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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