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Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $127 | 5 days | |
5 mg | $249 | 5 days | |
25 mg | $763 | 6-8 weeks | |
50 mg | $992 | 6-8 weeks | |
100 mg | $1,490 | 6-8 weeks | |
1 mL x 10 mM (in DMSO) | $287 | 5 days |
Description | CAL-130 Hydrochloride 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 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. Candidate animals for survival studies are ill-appearing, have a white blood cell count above 45,000/μL, 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 to 7.5 days for the control group. |
Molecular Weight | 462.94 |
Formula | C23H23ClN8O |
Cas No. | 1431697-78-7 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (108.01 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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