PIK-90 is a novel and potent PI3K inhibitor with IC50 values of 11 nM, 350 nM, 18 nM and 58 nM for p110α, p110β, p110γ and p110δ respectively. Phosphoinositide 3-kinases (PI3Ks) are among the most frequently activated signaling pathways in cancer. Inhibition with p110alpha inhibitor PIK-90 resulted in a significant reduction of chemotaxis and actin polymerization to CXCL12 and reduced migration beneath MSC (pseudoemperipolesis). In suspension and MSC cocultures, PIK-90 was potent inducers of CLL cell apoptosis.
Cell Experiment | |
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Cell lines | LN229:EGFR (PTENwt) and U87:EGFR (PTENmt) cells |
Preparation method | Cell proliferation assay and flow cytometry. For viability, 105 cells were seeded in 12-well plates in the presence of erlotinib, PI-103, PIK-90, rapamycin, erlotinib plus PIK-90, erlotinib plus rapamycin, erlotinib plus PIK-90, and rapamycin or erlotinib plus PI-103 for 72 h. Cell viability was determined using a WST-1 assay (Roche Molecular Biochemicals). |
Concentrations | 0, 0.1, 0.5, 1µM |
Incubation time | 72h |
Animal Experiment | |
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Animal models | Human primary GBM43 cells female BALB/c nu/nu mice bearing xenografts model |
Formulation | DMSO:H20 |
Dosages | 40 mg/kg |
Administration | daily i.p. |
Molecular Weight | 351.36 |
Formula | C18H17N5O3 |
CAS Number | 677338-12-4 |
Solubility (25°C) | DMSO |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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