A66 是高效的、特异性的、选择性 p110α 抑制剂，其 IC50=32 nM。

A66 is a specific and effective p110α inhibitor(IC50=32 nM).

在雄性CD1小鼠体内,A66（10 mg/kg）在丙酮酸盐耐量测试中增加葡萄糖产生.在SK-OV-3肿瘤组织中,A66（100 mg / kg）能够降低Akt/PKB 和p70 S6激酶的磷酸化,抑制肿瘤细胞生长.

对于p110α的致癌形式,如p110αE545K（IC50=30 nM）和p110αH1047R（IC50=43 nM）,A66能够显著抑制其发挥作用。

IC50 values are evaluated using the PI3K (human) HTRF Assay. p85α/p110δ is obtained from Invitrogen. All other isoforms are produced in-house by co-expressing full-length human p85α with the indicated human full-length catalytic subunit containing a histidine tag at the N-terminus to allow purification. The PI3Ks are titrated and used at a concentration between their EC65-EC80 values. PI3K activity in immunoprecipitates is assayed using an antibody to the N-SH2 (N-Src homology 2) domain of p85α. Assays for other lipid kinases and protein kinases are performed by the National Centre for Protein Kinase Profiling and Invitrogen Drug Discovery Services[1].

1166227-08-2

C17H23N5O2S2

393.52

DMSO:79 mg/mL (200.74 mM)
H2O:<1 mgml
Ethanol:1 mg/mL (2.54 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years