Serum stability of 67Cu chelates: Comparison with 111In and 57Co

William C. Cole; Sally J. DeNardo; Claude F. Meares; Michael J. McCall; Gerald L. DeNardo; Alan L. Epstein; Harold A. O'Brien; Min K. Moi

doi:10.1016/0883-2897(86)90011-5

Serum stability of ⁶⁷Cu chelates: Comparison with ¹¹¹In and ⁵⁷Co

William C. Cole, Sally J. DeNardo, Claude F. Meares, Michael J. McCall, Gerald L. DeNardo, Alan L. Epstein, Harold A. O'Brien, Min K. Moi

Chemistry

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Abstract

Simple chelates and chelate conjugated monoclonal antibodies labeled with ¹¹¹In, ⁵⁷Co and ⁶⁷Cu demonstrate marked differences in stability when exposed to a serum environment. Among these radiometals, on DTPA, the order of stability is ¹¹¹In ⁵⁷Co ≫ ⁶⁷Cu. On benzyl-EDTA, the order of stability is ¹¹¹In {reversed tilde equals} ⁵⁷Co ≫ ⁶⁷Cu. Among those investigated, the only serum stable ⁶⁷Cu chelate found was ⁶⁷Cu-TETA. The order of stability observed for ⁵⁷Co vs ⁶⁷Cu is contrary to published equilibrium constants. These in vitro studies suggest that the in vivo behavior of metal chelates exposed to a complex molecular environment may not be predicted by classically determined equilibrium constants.

Original language	English (US)
Pages (from-to)	363-368
Number of pages	6
Journal	International Journal of Radiation Applications and Instrumentation.
Volume	13
Issue number	4
DOIs	https://doi.org/10.1016/0883-2897(86)90011-5
State	Published - 1986

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Serum stability of ⁶⁷Cu chelates : Comparison with ¹¹¹In and ⁵⁷Co. / Cole, William C.; DeNardo, Sally J.; Meares, Claude F.; McCall, Michael J.; DeNardo, Gerald L.; Epstein, Alan L.; O'Brien, Harold A.; Moi, Min K.

In: International Journal of Radiation Applications and Instrumentation., Vol. 13, No. 4, 1986, p. 363-368.

Research output: Contribution to journal › Article › peer-review

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title = "Serum stability of 67Cu chelates: Comparison with 111In and 57Co",

abstract = "Simple chelates and chelate conjugated monoclonal antibodies labeled with 111In, 57Co and 67Cu demonstrate marked differences in stability when exposed to a serum environment. Among these radiometals, on DTPA, the order of stability is 111In 57Co ≫ 67Cu. On benzyl-EDTA, the order of stability is 111In {reversed tilde equals} 57Co ≫ 67Cu. Among those investigated, the only serum stable 67Cu chelate found was 67Cu-TETA. The order of stability observed for 57Co vs 67Cu is contrary to published equilibrium constants. These in vitro studies suggest that the in vivo behavior of metal chelates exposed to a complex molecular environment may not be predicted by classically determined equilibrium constants.",

author = "Cole, {William C.} and DeNardo, {Sally J.} and Meares, {Claude F.} and McCall, {Michael J.} and DeNardo, {Gerald L.} and Epstein, {Alan L.} and O'Brien, {Harold A.} and Moi, {Min K.}",

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doi = "10.1016/0883-2897(86)90011-5",

language = "English (US)",

volume = "13",

pages = "363--368",

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T1 - Serum stability of 67Cu chelates

T2 - Comparison with 111In and 57Co

AU - Cole, William C.

AU - DeNardo, Sally J.

AU - Meares, Claude F.

AU - McCall, Michael J.

AU - DeNardo, Gerald L.

AU - Epstein, Alan L.

AU - O'Brien, Harold A.

AU - Moi, Min K.

PY - 1986

Y1 - 1986

N2 - Simple chelates and chelate conjugated monoclonal antibodies labeled with 111In, 57Co and 67Cu demonstrate marked differences in stability when exposed to a serum environment. Among these radiometals, on DTPA, the order of stability is 111In 57Co ≫ 67Cu. On benzyl-EDTA, the order of stability is 111In {reversed tilde equals} 57Co ≫ 67Cu. Among those investigated, the only serum stable 67Cu chelate found was 67Cu-TETA. The order of stability observed for 57Co vs 67Cu is contrary to published equilibrium constants. These in vitro studies suggest that the in vivo behavior of metal chelates exposed to a complex molecular environment may not be predicted by classically determined equilibrium constants.

AB - Simple chelates and chelate conjugated monoclonal antibodies labeled with 111In, 57Co and 67Cu demonstrate marked differences in stability when exposed to a serum environment. Among these radiometals, on DTPA, the order of stability is 111In 57Co ≫ 67Cu. On benzyl-EDTA, the order of stability is 111In {reversed tilde equals} 57Co ≫ 67Cu. Among those investigated, the only serum stable 67Cu chelate found was 67Cu-TETA. The order of stability observed for 57Co vs 67Cu is contrary to published equilibrium constants. These in vitro studies suggest that the in vivo behavior of metal chelates exposed to a complex molecular environment may not be predicted by classically determined equilibrium constants.

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ER -

Serum stability of ⁶⁷Cu chelates: Comparison with ¹¹¹In and ⁵⁷Co

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