526560
PI 3-Kδ/γ Inhibitor XV, SW-14
The PI 3-Kδ/γ Inhibitor XV, SW-14 controls the biological activity of PI 3-Kδ/γ. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonym(s):
PI 3-Kδ/γ Inhibitor XV, SW-14, 2-((4-amino-3-(3-fluoro-4-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)methyl)-5-methyl-3-o-tolylquinazolin-4(3H)-one, PI 3-K Inhibitor XV
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About This Item
Empirical Formula (Hill Notation):
C28H22FN7O2
Molecular Weight:
507.52
UNSPSC Code:
12352200
Assay:
>95% (HPLC)
Form:
powder
Storage condition:
OK to freeze
Quality Segment
assay
>95% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
white
solubility
DMSO: 100 mg/mL
shipped in
ambient
storage temp.
−20°C
General description
A cell permeable, ATP competitive tolyl quinazolinone inhibitor of PI 3-Kδ/γ that displays 70-fold selectivity over PI 3-Kβ and 900-fold selectivity over PI 3-Kα in enzymatic assays with an IC50 = 9 nM for PI3Kδ and 21 nM for PI 3-Kγ and in a cell-based assay with an EC50 = 132 nM for PI 3-Kδ and 4.5 nM for PI 3-K γ. It elicits an inflammatory marker suppression effect in co-cultures of HUVEC and PBMCs stimulated with lipopolysacharide. Additionally, TNFα production decreases dose-dependently in the same cell lines treated with 370 nM to 10 µM of compound. SW14 exhibits a stronger effect compared to that of PI 3-Kδ inhibition (SW30) or pan-PI 3-K inhibition with different anti-inflammatory profile. In contrast to PI 3-Kα/β it also shows very little anti-proliferative effects even at the highest dose tested (10 µM) in HUVEC culture only.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Williams, O., et al. 2010. Chem Biol.17, 123.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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