3-(4-Morpholinothieno[3,2-d]pyrimidin-2-yl)phenol, 2HCl Off-white solid. PROTECT FROM LIGHT. HYGROSCOPIC. PACKAGED UNDER INERT GAS. A cell-permeable morpholino-thienopyrimidine compound that acts as a potent and isoform-selective inhibitor of PI 3-kinases (IC50 = 2 nM, 16 nM, 660 nM, and 220 nM for p110a, p110b p110g, and PI 3-K C2b, respectively) and inhibits non-PI 3-K kinases only at much higher concentrations (IC50 ≥3.4 µM for Cdk2/E, KDR, PKA, and PKCa). Shown to inhibit cell proliferation (IC50 = 580 nM) and serum-stimulated Akt phosphorylation (IC50 <3 µM) in A375 melanoma cells. Purity: ≥95% by HPLC. Ref.: Hayakawa, M., et al. 2006. Bioorg. Med. Chem. 14, 6847. |
