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| Product Name: | A66 | | Synonyms: | (2S)-N1-[2-(tert-Butyl)-4'-methyl[4,5'-bithiazol]-2'-yl]-1,2-pyrrolidinedicarboxamide;CS-435;(2S)-N1-(5-(2-tert-butylthiazol-4-yl)-4-methylthiazol-2-yl)pyrrolidine-1,2-dicarboxamide;(2S)-N1-[2-(tert-Butyl)-4'-methyl[4,5'-bithiazol]-2'-yl]-1,2-pyrrolidinedicarboxamide A 66;A66, 98%, a potent and specific p110α inhibitor;(2S)-N1-[2-(1,1-Dimethylethyl)-4'-methyl[4,5'-bithiazol]-2'-yl]-1,2-pyrrolidinedicarboxamide;A 66;A-66;1,2-Pyrrolidinedicarboxamide, N1-[2-(1,1-dimethylethyl)-4'-methyl[4,5'-bithiazol]-2'-yl]-, (2S)- | | CAS: | 1166227-08-2 | | MF: | C17H23N5O2S2 | | MW: | 393.53 | | EINECS: | | Product Categories: | Inhibitors;Akt;PI3K;PI3K/Akt/mTOR;mTOR | | Mol File: | 1166227-08-2.mol |
| 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) |
| 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. | | 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. |
| A66 Preparation Products And Raw materials |
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