900185-02-6
900185-02-6 structure
- Name: PIK-294
- Chemical Name: 2-[[4-amino-3-(3-hydroxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]methyl]-5-methyl-3-(2-methylphenyl)quinazolin-4-one
- CAS Number: 900185-02-6
- Molecular Formula: C28H23N7O2
- Molecular Weight: 489.528
- Catalog: Biochemical Inhibitor PI3K/Akt/mTOR inhibitor (PI3K/Akt/mTOR) PI3K inhibitor
- Create Date: 2018-12-30 13:17:13
- Modify Date: 2024-01-04 18:26:26
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PIK-294 is a potent p110δ-selective inhibitor with an IC50 of 10 nM.
| Name | 2-[[4-amino-3-(3-hydroxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]methyl]-5-methyl-3-(2-methylphenyl)quinazolin-4-one |
|---|---|
| Synonyms |
2-{[4-Amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]methyl}-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone
4(3H)-Quinazolinone, 2-[[4-amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]methyl]-5-methyl-3-(2-methylphenyl)- cc-610 S2227_Selleck 2-((4-amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)methyl)-5-methyl-3-o-tolylquinazolin-4(3H)-one PIK 294,PIK294 PIK-294 |
| Description | PIK-294 is a potent p110δ-selective inhibitor with an IC50 of 10 nM. |
|---|---|
| Related Catalog | |
| Target |
p110δ:10 nM (IC50) p110γ:160 nM (IC50) p110β:490 nM (IC50) p110α:10 μM (IC50) |
| In Vitro | Analysis of the specific Class I PI3 Kinase catalytic isoforms p110α (IC50=10 μM), p110β (IC50=0.49 μM), p110δ (IC50=0.01 μM) and p110γ (IC50=0.16 μM) using the inhibitor PIK-294 indicates differential roles in CXCL8-induced neutrophil migration. PIK-294 inhibits both chemokinetic and chemotactic CXCL8-induced migration[1]. When cells are pre-treated with the PI3Kδ selective inhibitor PIK-294, CXCL8-induced migration in the non-gradient and the gradient assay is significantly inhibited. PIK-294 is used at two concentrations 1 μM and 10 μM. Pre-treatment with 1 μM inhibits migration to a greater extent in the non-gradient assay than in the gradient assay. Pre-treatment with 10 μM inhibits migration to a significantly greater extent than the lower dose in both assays. Prior to stimulation with CXCL8, pre-treatment of the cells with the PI3K inhibitors, Wortmannin (50 nM), PIK-294 (10 μM) and AS-605240 (10 μM) for 2 minutes, cause a reduction in the phosphorylation of Akt. Pre-treatment of cells prior to stimulation with GM-CSF and the DMSO control with the PI3K inhibitors Wortmannin (50 nM), PIK-294 (10 μM) and AS-605240 (10 μM) for 2 minutes, reduce the phosphorylation of Akt (p<0.05 for inhibition of PI3Kδ)[2]. |
| Cell Assay | Neutrophils at a concentration of 6×106 cells/mL are pre-treated with 1 μM and 10 μM of the PIK-294 for 30 mins prior to the addition of CXCL8 (100 ng/mL) or 0.5 ng/mL GM-CSF. Then a non-gradient or gradient gel assay depending on the type of migration is performed. The gels are then constructed and the migration studied[2]. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 790.4±70.0 °C at 760 mmHg |
| Molecular Formula | C28H23N7O2 |
| Molecular Weight | 489.528 |
| Flash Point | 431.8±35.7 °C |
| Exact Mass | 489.191315 |
| PSA | 124.74000 |
| LogP | 3.34 |
| Vapour Pressure | 0.0±2.9 mmHg at 25°C |
| Index of Refraction | 1.753 |
| Storage condition | -20℃ |
| Symbol |
GHS06 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H301 |
| Precautionary Statements | P301 + P310 + P330 |
| RIDADR | UN 2811 6.1 / PGIII |