Description: Potent and selective PI 3-kinase p110δ inhibitor
Chemical Name: 6-[[4-(Cyclopropylmethyl)-1-piperazinyl]methyl]-2-(5-fluoro-1H-indol-4-yl)-4-(4-morpholinyl)-thieno[3,2-d]pyrimidine
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Potent and selective PI 3-kinase p110δ inhibitor (IC50 = 5 nM; Ki = 1.5 nM). Exhibits >100-fold selectivity over p100α, p100γ and p100β isoforms (IC50 values are 600, 910, >10,000 nM, respectively). Attenuates 4TI tumor growth and metastasis in vivo.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
10.13
20
Preparing Stock Solutions
The following data is based on the product molecular weight 506.64. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
1.97 mL
9.87 mL
19.74 mL
5 mM
0.39 mL
1.97 mL
3.95 mL
10 mM
0.2 mL
0.99 mL
1.97 mL
50 mM
0.04 mL
0.2 mL
0.39 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Aliet al (2014) Inactivation of PI(3)K p110δ breaks regulatory T-cell-mediated immune tolerance to cancer. Nature 510 407 PMID: 24919154
Portaet al (2014) Targeting PI3K/Akt/mTOR signaling in cancer. Front.Oncol. 4 64 PMID: 24782981