. Author manuscript; available in PMC: 2013 Oct 19.

Published in final edited form as: Recent Results Cancer Res. 2013;194:149–175. doi: 10.1007/978-3-642-27994-2_9

Table 1.

α-MSH Peptide Analogs with Competitive Binding Assay and Stability Data.

Peptide	Sequence	Mass (obs/calc)	IC₅₀ (nM)	24 hour stability (% remaining)
a-MSH	Ac-SYSMEHFRWGKPV-NH2	1664.7/1664.9	2.1 ±0.4	N.D.
DOTA-a-MSH	DOTA-SYSMEHFRWGKPV-NH2	2009.0/2009.3	1.8 ±0.3	7.4
NDP-a-MSH	Ac-SYS-Nle-EHfRWGKPV-NH2	1646.6/1646.9	0.21 ±0.03	N.D.
DOTA-NDP-a-MSH	DOTA-SYS-Nle-EHfRWGKPV-NH2	1990.6/1991.2	0.59 ±0.11	41
MTII	Ac-Nle-cyclo[DHfRWK]-NH2	1024.6/1024.2	0.26 ±0.08	N.D.
ClickMTII	Ac-Nle-cyclo[Pra-HfRW-Lys(N₃)]-NH2	1048.3/1048.2	0.39 ±0.06	N.D.
DOTA-ClickMTII	DOTA-Nle-cyclo[Pra-HfRW-Lys(N₃)]-NH2	1392.3/1392.6	25 ±1	100
DOTA-GG-ClickMTII	DOTA-GG-Nle-cyclo[Pra-HfRW-Lys(N₃)]-NH2	1506.1/1506.7	2.7 ±0.8	99
ClickMTII-K-DOTA	Ac-Nle-cyclo[Pra-HfRW-Lys(N₃)]-K(DOTA)-NH2	1562.4/1562.8	1.4 ±0.2	99
ClickMTII-GGK-DOTA	Ac-Nle-cyclo[Pra-HfRW-Lys(N₃)]-GGK(DOTA)-NH2	1676.6/1676.9	1.1 ±0.2	100