A66

    • Catalog No.:MC0545
      • CasNo:
      • 1166227-08-2
      • MolecularFormula:
      • C17H23N5O2S2
      • Purity:
      • >98%
      • Target:
      • PI3K
      • IC50:
      • IC50: 32 nM (p110α), 30 nM (p110α E545K), 43 nM (p110α H1047R), 3480 nM (p110γ)[1]
      • In Vitro:
      • A66 is a potent inhibitor of the wild-type and oncogenic forms of p110α but not other class-I PI3K isoforms[1]. The p110α-specific inhibitor A66 (0.7 μM) induces a 75-80% reduction in focus formation by the highly transforming iSH2 mutants KS459delN, DKRMNS560del, and K379E. The p110α-specific inhibitor A66 reduced phosphorylation of Akt on T308 by all p85 mutants[2].
      • In Vivo:
      • The optimal dosing strategy for xenograft studies is determined by investigating the drug pharmacokinetics after a dose of 10 mg/kg of body weight by intraperitoneal injection in CD-1 mice. Despite a short half-life of only 0.42 h, the large Cmax (8247 nM) of A66 S that is reached 30 min after dosing ensured that the AUC0-inf (area under the curve from zero time to infinity) (6809 nM•h) is similar to that of BEZ-235 (7333 nM•h), which has a longer half-life of 2.73 h. Furthermore, the A66 on SK-OV-3 tumour tissue is tested using a single dose of 100 mg/kg of body weight to determine whether a long-lasting effect of the drug could be achieved on target tissues. These studies show that A66 causes a profound reduction in the phosphorylation of Akt/PKB and p70 S6 kinase, but not of ERK (extracellular-signal-regulated kinase), at both 1 and 6 h after dosing. Levels of A66 in plasma are determined to be 21.1±1.2 μM and 9.1±1.1 μM at 1 and 6 h after drug injection, whereas levels of A66 in th
      • Fields:
      • A66 is a potent and specific p110α inhibitor with IC50 of 32 nM, >100 fold selectivity for p110α over other class-I PI3K isoforms.
      • Specificity:
      • Target: PI3K. Fields: A66 is a potent and specific p110α inhibitor with IC50 of 32 nM, >100 fold selectivity for p110α over other class-I PI3K isoforms.
      • Source:
      • Rabbit
      • Dilution:
      • IC50: 32 nM (p110α), 30 nM (p110α E545K), 43 nM (p110α H1047R), 3480 nM (p110γ)[1]
      • Concentration:
      • >98%
      • Storage Stability:
      • 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
      • MolecularWeight(Da):
      • 393.53
      • References:
      • [1]. Jamieson S, et al. A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types. Biochem J, 2011, 438(1), 53-62. [2]. Sun M, et al. Cancer-
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