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PIK-294 is a highly selective p110 inhibitor with an IC50 of 3 nM. PI3K contains a m-phenol and a pyrazolopyrimidine core. When PIK-294 is compared to tyrosine kinase–selective pyrazolopyrimidines such as PP20, the two molecules span more than 108 fold in relative target selectivity. PIK-294 is 20- to 60-fold more potent than the parent compound, PIK-293, making PIK-294 one of the most potent p110δ- selective inhibitors that has been reported. PIK-294 also inhibits p110α, p110β, p110γ, DNA-PK and mTOR with IC50 of 9.6, 0.67, 0.2, 48 and >50 µM.
| Molecular Weight | 489.53 |
| Formula | C28H23N7O2 |
| CAS Number | 900185-02-6 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PI3K Products |
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| PI3Kγ inhibitor AZ2
PI3Kγ inhibitor AZ2 is a highly selective PI3Kγ inhibitor (The pIC50 value for PI3Kγ is 9.3). |
| NIBR-17
NIBR-17 is a pan-class I PI3K inhibitor with suitable pharmacokinetic properties and inhibits tumor growth. |
| RV-1729
RV-1729 is an inhibitor of the phosphatidylinositol 3-kinase-δ (PI3Kδ). |
| Vulolisib
Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. |
| Vps34-IN-4
Vps34-IN-4 is a potent, selective, and orally active inhibitor of VPS34. |
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