PIK-294

Cas：900185-02-6

Product Information：

PIK-294 is a highly selective inihibitor of the phosphoinositide 3-kinase (PI3K) p110δ with an IC50 value of 10 nM compared to IC50 values of 10 μM, 490 nM and 160 nM for PI3Kα/β/γ, respectively. PIK-294 has been used to help distinguish the unique roles of the various PI3-K isoforms. PIK-294 inhibited both chemokinetic and chemotactic CXCL8-induced migration.

Chemical Formula: C28H23N7O2

Exact Mass: 489.19

Molecular Weight: 489.52792

Elemental Analysis: C, 68.70; H, 4.74; N, 20.03; O, 6.54

Synonym: 

PIK294

PIK 294

PIK-294

Chemical Name:

2-((4-amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)methyl)-5-methyl-3-(o-tolyl)quinazolin-4(3H)-one

InChi Key:

WFSLJOPRIJSOJR-UHFFFAOYSA-N

InChi Code:

InChI=1S/C28H23N7O2/c1-16-7-3-4-12-21(16)35-22(32-20-11-5-8-17(2)23(20)28(35)37)14-34-27-24(26(29)30-15-31-27)25(33-34)18-9-6-10-19(36)13-18/h3-13,15,36H,14H2,1-2H3,(H2,29,30,31)

Smiles Code:

O=C1N(C2=CC=CC=C2C)C(CN3N=C(C4=CC=CC(O)=C4)C5=C(N)N=CN=C53)=NC6=C1C(C)=CC=C6]

Technical Data：

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

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. 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).

References：

1. Inhibitors of the PI3k/Akt/Ikk/NF-kb signalling pathway, pharmaceutically acceptable salts thereof and compositions containing said inhibitors for prophylaxis and treatment of viral diseases. Fedichev, Petr Olegovich; Vinnik, Andrey Alexandrovich. PCT Int. Appl. (2013), WO 2013147649 A2 20131003 .

2. Methods for predicting cancer treatment responsiveness to phosphatidylinositol 3-kinase (PI3K) inhibitors. Jane, Stephen M.; Darido, Charbel. PCT Int. Appl. (2013), WO 2013029116 A1 20130307.

3. Methods for treating oncovirus positive cancers. Jimeno, Antonio; Hausman, Diana F.; Peterson, Scott. PCT Int. Appl. (2012), WO 2012118978 A1 20120907.

4. Use of phosphatidylinositol-3'-kinase (PI3K) p110 delta isoform inhibitors for treating retroviral infection and replication. Katsikis, Peter D.; Boesteanu, Alina C.; Turner, Martin. PCT Int. Appl. (2012), WO 2012009452 A1 20120119.

5. Methods and compositions for treatment of ophthalmic conditions. Wilson, Troy Edward; Rommel, Christian; Liu, Yi; Ren, Pingda. PCT Int. Appl. (2010), WO 2010059593 A1 20100527.

Products are for research use only. Not for human use.