4-(4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-methyl-1H-pyrazol-3-yl)-6-ethylresorcinol White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable pyrazoloresorcinol compound that inhibits HSP90 ATPase activity (IC50 = 3.2 µM and 6.6 µM against human HSP90b and yeast HSP90, respectively) by targeting the enzyme's N-terminal ATP binding site. It exhibits no detectable effects against human Hsp70 or topoisomerase II even at concentrations as high as 100 µM and inhibits a panel of 20 commonly studied kinases only at much higher concentrations. Unlike 17-AAG (Cat. No. 100068), the antitumor activity of CCT018159 is not affected by the expression of NQ01/DT-diaphorase or P-glycoprotein. Purity: ≥98% by HPLC. CAS 171009-07-7. Ref.: Hardcastle, A., et al. 2007. Mol. Cancer Ther. 6, 1112. Sharp, S.Y., et al. 2007. Cancer Res. 67, 2206. Smith, N.F., et al. 2006. Mol. Cancer Ther. 5, 1628. Dymock, B.W., et al. 2005. J. Med. Chem. 48, 4212. Cheung, K.M., et al. 2005. Bioorg. Med. Chem. Lett. 15, 3338.
R: 36/37/38; S: 24/25-36/37/39 |
