CAS | 496849-46-8 |
Sequence | H-Tyr-cyclo(-D-Dab-Arg-Phe-Phe-D-Trp-Lys-Thr-Phe) |
Sequence Single | Y-cyclo(-D-Dab-RFFwKTP) |
Molecular Formula | C67H85N15O11 |
Molecular Weight | 1276.51 |
Synonyms | KE 108 |
Technology | Synthetic |
Storage | -20°C, avoid light, cool and dry place |
Application | Cancer Research |
Description | Tyr-(D-Dab4,Arg5,D-Trp8)-cyclo-Somatostatin-14 (4-11) also called KE 108, is a high affinity ligand for all five somatostatin receptors (sst1-sst5). In AtT-20 mouse anterior pituitary tumor cells which mainly express sst2 and sst5 receptors the binding affinity of this somatostatin analog was found to be higher than that of somatostatin-14 and octreotide. In a model of epileptogenesis, however, KE 108 did not exhibit antiepileptic activity suggesting that the high potency and efficacy of a synthetic ligand to all known somatostatin receptors may not reproduce entirely the effects of the natural ligand. |
References | 1. Arginine-rich molecular transporters for drug delivery: role of backbone spacing in cellular uptake. J.B.Rothbard et al., J. Med. Chem., 45, 3612 (2002) |