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CAL-130 Hydrochloride is a PI3Kδ and PI3Kγ inhibitor (IC50s: 1.3 and 6.1 nM).
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). |
Targets&IC50 | p110β:56 nM, p110α:115 nM, p110γ:6.1 nM, p110δ:1.3 nM |
In vitro | CAL-130 selectively inhibits the catalytic domains of p110γ and p110δ with IC50s of 1.3 and 6.1 nM, respectively (115 and 56 nM for p110α and p110β), and does not affect other intracellular signaling pathways essential for cell function and survival, such as p38 MAPK or insulin receptor tyrosine kinase. |
In vivo | The clinical significance of inhibiting PI3Kγ and PI3Kδ activities is assessed by administering CAL-130 to Lck/Ptenfl/fl mice with established T cell acute lymphoblastic leukemia. Candidate mice, exhibiting illness, a white blood cell count above 45,000/μL, blasts on peripheral smear, and >75% Thy1.2 and Ki-67 double-positive circulating cells, receive an oral dose (10 mg/kg) of CAL-130 every 8 hours for 7 days and are monitored until moribund. Despite the limited duration of therapy, CAL-130 effectively extends median survival to 45 days 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 | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (108.01 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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