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PIK 90
- Moderately soluble in DMSO with 0.1N HCl(aq)
- MF: C18H17N5O3
- MW: 351.36
Description
PIK 90 is a cell-permeable class I phosphoinositide 3-kinase (PI3K) inhibitor with strongest activity at PI3K p110α (IC50 value of 11 nM) and additional inhibition of p110γ, p110δ and p110β with IC50 values of 18, 58, 350 nM, respectively, and low mTOR activity.
PIK 90 suppresses PI3K-dependent PIP3 production and downstream AKT signaling while showing comparatively weak activity at mTOR. Its isoform profile makes it useful for dissecting class I PI3K signaling in growth, survival and immune pathways.
Key Features
- Potent class I PI3K inhibitor
- IC50: 11 nM (p110α), 18 nM (p110γ), 58 nM (p110δ) and 350 nM (p110β)
- Low activity against mTOR relative to class I PI3K isoforms
- Cell-permeable tool for PI3K–AKT pathway inhibition
Applications
- PI3K isoform profiling
- PIP3 and AKT signaling studies
- Cancer cell growth and survival models
- Immune-cell and inflammatory signaling research
More Information
| Parent CAS No. | 677338-12-4 |
|---|---|
| Chemical Name | N-(7,8-Dimethoxy-2,3-dihydro-imidazo[1,2-c]quinazolin-5-yl)-nicotinamide |
| SMILES | C1C=C2C3=NCCN3C(NC(=O)C3C=NC=CC=3)=NC2=C(OC)C=1OC |
| MFCD | MFCD12546131 |
| InChi | InChI=1S/C18H17N5O3/c1-25-13-6-5-12-14(15(13)26-2)21-18(23-9-8-20-16(12)23)22-17(24)11-4-3-7-19-10-11/h3-7,10H,8-9H2,1-2H3,(H,21,22,24) |
| InChiKey | ZJAVHOMVDCMAMF-UHFFFAOYSA-N |
| CID | 135398491 |
| Short Description | PI3K p110α inhibitor |
References
- JS Chen et al. Characterization of structurally distinct, isoform-selective phosphoinositide 3′-kinase inhibitors in combination with radiation in the treatment of glioblastoma. Mol. Cancer Ther. 2008, 7, 841-850.
- ZA Knight et al. A Pharmacological Map of the PI3-K Family Defines a Role for p110α in Insulin Signaling. Cell 2006, 125, 733–747.
- C Chaussade et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007, 404(3), 449–458.
- S Kim et al. Insulin-like growth factor-1 regulates platelet activation through PI3-Kα isoform. Blood, 2007, 110(13), 4206-4213.
- List of publications using PIK 90 (Axon 1362) purchased from Axon Medchem
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