White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. An antifungal macrocyclic lactone antibiotic that acts as a protein tyrosine kinase inhibitor. Inhibits p60^v-src kinase activity (IC₅₀ = 0.27 nM). Inhibits the expression of COX-2 (IC₅₀ = 27 nM) without affecting COX-1 expression in LPS-stimulated macrophages. Disrupts K-Ras-activated signaling pathways by selectively depleting Raf kinase. Inhibits tyrosine phosphorylation of p53/56^lyn in LPS-stimulated macrophages. Suppresses NIH/3T3 cell transformation by diverse oncogenes such as src, ras, and mos in part by blocking the key signal transduction intermediates such as MAP kinase and GAP-associated p62. Also exhibits anti-angiogenic activity in vivo. Purity: ≥97% by TLC. RTECS RR1105000, CAS 12772-57-5.

Merck Index: 14, 6253
Ref.: Soga, S., et al. 1998. J. Biol. Chem. 273, 822. Chanmugam, P., et al. 1995. J. Biol. Chem. 270, 5418. Shimada, Y., et al. 1995. J. Antibiot. 48, 824. Zhao, J.F., et al. 1995. Oncogene 11, 161. Oikawa, T., et al. 1993. Eur. J. Pharmacol. 241, 221. Kwon, H.J., et al. 1992. Cancer Res. 52, 6926.
R: 20/21/22-36/37/38; S: 26-36