A selective p110α inhibitor
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A-66

Item No. 17382

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S)-N1-[2-(1,1-dimethylethyl)-4'-methyl[4,5'-bithiazol]-2'-yl]-1,2-pyrrolidinedicarboxamide
CAS Number
1166227-08-2
Molecular Formula
C17H23N5O2S2
Formula Weight
393.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
306 nm
SMILES
CC1=C(C2=CSC(C(C)(C)C)=N2)SC(NC(N3CCC[C@H]3C(N)=O)=O)=N1
InChi Code
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
InChi Key
HBPXWEPKNBHKAX-NSHDSACASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    A-66 is a potent, selective inhibitor of the PI3K isoform p110α (IC50 = 32 nM in a cell-free assay).1 It displays over 100-fold selectivity for p110α over other isoforms. A-66 is effective in vivo, suppressing the growth of SKOV3 tumor xenografts in mice.1 It also impairs all measures of in vivo insulin action in mice.2 A-66 partially suppresses B cell receptor-dependent Akt activation and proliferation.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jamieson, S., Flanagan, J.U., Kolekar, S., et al. A drug targeting only p110a can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types. Biochem. J. 438(1), 53-62 (2011).

    2. Smith, G.C., Ong, W.K., Rewcastle, G.W., et al. Effects of acutely inhibiting PI3K isoforms and mTOR on regulation of glucose metabolism in vivo. Biochem. J. 442(1), 161-169 (2012).

    3. So, L., Yea, S.S., Oak, J.S., et al. Selective inhibition of phosphoinositide 3-kinase p110α preserves lymphocyte function. The Journal of Biological Chemisty 288(8), 5718-5731 (2013).