A66 Chemical Properties

Density 

1.354

storage temp. 

Sealed in dry,Store in freezer, under -20°C

solubility 

insoluble in H2O; ≥19.7 mg/mL in DMSO; ≥2.63 mg/mL in EtOH with gentle warming

form 

solid

pka

6.27±0.70(Predicted)

Safety Information

HS Code 

29341000

A66 Usage And Synthesis

Description

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

Uses

A66 is a potent and specific p110α inhibitor. Inhibition of p110α can block phosphoinositide 3-kinase (PI3K) signalling and tumor growth in certain cell types.

Definition

ChEBI: (2S)-N1-[5-(2-tert-butyl-4-thiazolyl)-4-methyl-2-thiazolyl]pyrrolidine-1,2-dicarboxamide is a proline derivative.

Enzyme inhibitor

This potent and highly selective p110α inhibitor (FW = 393.53; CAS 1166227-08-2; Solubility: 79 mg/mL DMSO, 1 mg/mL H2O), also known as (2S)-N1-(5-(2-tert-butylthiazol-4-yl)-4-methylthiazol-2-yl)pyrrolidine-1, 2-dicarboxamide, has a IC50 value of 32 nM for the wild-type phosphoinositide-3 kinase p110 α as well as oncogenic forms of p110α such as p110α E545K (IC50 = 43 nM) and p110α H1047R (IC50 = 43 nM). A66 inhibition also demonstrated that cancer-specific mutations in the iSH2 (inter-SH2) and nSH2 (N-terminal SH2) domains of p85α, the regulatory subunit of phosphatidylinositide 3-kinase (PI3K), show gain of function, inducing oncogenic cellular transformation, stimulating cellular proliferation, and enhancing PI3K signaling.

storage

Store at -20°C

A66(1166227-08-2)Related Product Information

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• 4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]-