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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 for A66
A66 is a 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 for A66
A66 is also offered as part of the Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for A66
| 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 for A66
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 39.35 | 100 |
Preparing Stock Solutions for A66
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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Product Datasheets for A66
References for A66
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
If you know of a relevant reference for A66, please let us know.
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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
3 Citations for A66
Citations are publications that use Tocris products. Selected citations for A66 include:
Eugene et al (2020) Increased mitochondrial and lipid metabolism is a conserved effect of Insulin/PI3K pathway downregulation in adipose tissue. Sci Rep 10 3418 PMID: 32099025
Tania et al (2021) Growth and Viability of Cutaneous Squamous Cell Carcinoma Cell Lines Display Different Sensitivities to Isoform-Specific Phosphoinositide 3-Kinase Inhibitors. Int J Mol Sci 22 PMID: 33808215
Christos et al (2021) Dominant Role of PI3K p110α over p110β in Insulin and β-Adrenergic Receptor Signalling. Int J Mol Sci 22 PMID: 34884613
Do you know of a great paper that uses A66 from Tocris? Please let us know.
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