DC Chemicals Limited
China
Product Name: PIK-294
Price: $550.0/100mg $1000.0/250mg $1900.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

900185-02-6

900185-02-6 structure

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
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	Research Areas >> Cancer
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	[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.

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