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A 66
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C17H23N5O2S2
- MW: 393.53
Description
A 66 is a potent and selective PI3K p110α inhibitor with a reported IC50 value of 32 nM.
PI3K p110α is frequently activated in cancer through PIK3CA mutation or upstream receptor signaling and drives AKT-mTOR pathway activation. A 66 is a highly useful tool for distinguishing p110α-dependent signaling from other PI3K isoforms.
Key Features
- Selective PI3K p110α inhibitor
- IC50: 32 nM for p110α
- Highly selective over other PI3K isoforms and tested protein kinases
- Useful for defining p110α-specific pathway dependence
Applications
- PI3Kα/PIK3CA signaling research
- AKT pathway and phosphoinositide signaling assays
- Cancer cell proliferation and survival studies
- PI3K isoform selectivity profiling
More Information
| Parent CAS No. | 1166227-08-2 |
|---|---|
| Chemical Name | (S)-N1-(2-tert-butyl-4'-methyl-4,5'-bithiazol-2'-yl)pyrrolidine-1,2-dicarboxamide |
| SMILES | C1(C(C)(C)C)=NC(C2SC(NC(=O)N3CCC[C@H]3C(N)=O)=NC=2C)=CS1 |&1:17,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C17H23N5O2S2/c1-9-12(10-8-25-14(20-10)17(2,3)4)26-15(19-9)21-16(24)22-7-5-6-11(22)13(18)23/h8,11H,5-7H2,1-4H3,(H2,18,23)(H,19,21,24)/t11-/m0/s1 |
| InChiKey | HBPXWEPKNBHKAX-NSHDSACASA-N |
| CID | 42636535 |
| Short Description | PI3K inhibitor |
References
- S Jamieson et al. A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types. Biochem J. 2011, 438(Pt 1), 53–62.
- Ashley J. Waardenberg et al. Phosphoinositide 3-Kinase (PI3K(p110α)) Directly Regulates Key Components of the Z-disc and Cardiac Structure. J. Biol. Chem. 2011, 286, 30837-30846.
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