CAS 900185-02-6|PIK-294

Introduction:Basic information about CAS 900185-02-6|PIK-294, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NamePIK-294
CAS Number900185-02-6Molecular Weight489.528
Density1.4±0.1 g/cm3Boiling Point790.4±70.0 °C at 760 mmHg
Molecular FormulaC28H23N7O2Melting Point/
MSDSChineseUSAFlash Point431.8±35.7 °C
Symbol
GHS06
Signal WordDanger

Names

Name2-[[4-amino-3-(3-hydroxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]methyl]-5-methyl-3-(2-methylphenyl)quinazolin-4-one
SynonymMore Synonyms

PIK-294 BiologicalActivity

DescriptionPIK-294 is a potent p110δ-selective inhibitor with an IC50 of 10 nM.
Related CatalogResearch Areas >>Cancer
Target

p110δ:10 nM (IC50)

p110γ:160 nM (IC50)

p110β:490 nM (IC50)

p110α:10 μM (IC50)

In VitroAnalysis 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 AssayNeutrophils 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

[1]. Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47.

[2]. Martin KJ, et al. The role of phosphoinositide 3-kinases in neutrophil migration in 3D collagen gels. PLoS One. 2015 Feb 6;10(2):e0116250.

Chemical & Physical Properties

Density1.4±0.1 g/cm3
Boiling Point790.4±70.0 °C at 760 mmHg
Molecular FormulaC28H23N7O2
Molecular Weight489.528
Flash Point431.8±35.7 °C
Exact Mass489.191315
PSA124.74000
LogP3.34
Vapour Pressure0.0±2.9 mmHg at 25°C
Index of Refraction1.753
InChIKeyWFSLJOPRIJSOJR-UHFFFAOYSA-N
SMILESCc1ccccc1-n1c(Cn2nc(-c3cccc(O)c3)c3c(N)ncnc32)nc2cccc(C)c2c1=O
Storage condition-20℃

Safety Information

Symbol
GHS06
Signal WordDanger
Hazard StatementsH301
Precautionary StatementsP301 + P310 + P330
RIDADRUN 2811 6.1 / PGIII

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
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