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Description: Potent and selective PI 3-kinase p110α inhibitor
Chemical Name: (2S)-N1-[2-(1,1-Dimethylethyl)-4'-methyl[4,5'-bithiazol]-2'-yl]-1,2-pyrrolidinedicarboxamide
Purity: ≥98% (HPLC)
Biological Activity
Potent and selective PI 3-kinase p110α inhibitor (IC50 = 32 nM). Exhibits >100-fold selectivity for p110α over other PI 3-kinase isoforms. Inhibits Akt signaling and tumor growth in SK-OV-3 xenografts in mice.
Compound Libraries
A66 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 393.53 |
| Formula | C17H23N5O2S2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1166227-08-2 |
| PubChem ID | 42636535 |
| InChI Key | HBPXWEPKNBHKAX-NSHDSACASA-N |
| Smiles | CC(C)(C)C1=NC(C2=C(C)N=C(NC(N3[C@H](C(N)=O)CCC3)=O)S2)=CS1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 39.35 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 393.53. Batch specific molecular weights may vary from batch to batch due to the degree 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 | 2.54 mL | 12.71 mL | 25.41 mL |
| 5 mM | 0.51 mL | 2.54 mL | 5.08 mL |
| 10 mM | 0.25 mL | 1.27 mL | 2.54 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
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References
References are publications that support the biological activity of the product.
Jamieson et al (2011) A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types. Biochem. J. 438 53 PMID: 21668414
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Keywords: A66, A66 supplier, PI, 3-kinase, PI3K, phosphoinositide, inhibitors, potent, selective, inhibits, p110a, alpha, α, 3-Kinase, 5595, Tocris Bioscience
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