2-(1H-Benzo[d]imidazol-1-yl)-N-(5-methoxy-2-methylphenyl)-6-(2-morpholinoethoxy)pyrimidin-4-amine, hydrate Light yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable, ATP binding site-targeting, tri-substituted pyrimidine that acts as a Lck (lymphocyte specific kinase) inhibitor (IC50 = 867 nM; [ATP] = 10 µM). Shown to block IL-2 release in Jurkat E6-1 T cell line (IC50 = 1.27 µM) stimulated by CD3 cross-linking and PMA. Although less potent than Lck Inhibitor II (Cat. No. 428206), it exhibits much improved aqueous solubility (27 µg/ml in 50 mM PBS, pH 7.4, ionic strength 0.15 M) and in vivo bioavailability (F = 22%, p.o. and i.v. at 10 mg/kg). Purity: ≥97% by HPLC. Ref.: Sabat, M., et al. 2006. Bioorg. Med. Chem. Lett. 16, 5973. |
