Table 1 Summary of data for in vitro assays

From: Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity

 

Induction of AP activitya (% E2)

Relative ERα protein levelsb (% vehicle)

IC50 proliferationc (nM)

IC50 transcriptiond (nM)

endoxifen

73% ± 10 (n = 8)

139% ± 34 (n = 20)

13 ± 2.2 (n = 5)

6.3 ± 1.3 (n = 5)

fulvestrant

0.05% ± 2.7 (n = 58)

28% ± 12 (n = 40)

2.5 ± 0.3 (n = 45)

2.0 ± 0.2 (n = 41)

OP-1074

10% ± 4.4 (n = 29)

49% ± 13 (n = 15)

7.2 ± 0.9 (n = 26)

1.8 ± 0.3 (n = 17)

OP-1154

40% ± 6.5 (n = 3)

123% ± 22 (n = 4)

6.0 ± 1.1 (n = 5)

5.6 ± 2.1 (n = 4)

OP-1039

49% ± 18 (n = 8)

119% ± 13 (n = 6)

6.4 ± 1.0 (n = 10)

0.5 ± 0.1 (n = 9)

OP-1047

136% ± 15 (n = 4)

319% ± 100 (n = 5)

5.5 ± 1.4 (n = 3)

1.3 ± 0.4 (n = 3)

OP-1156

40% ± 7.8 (n = 3)

152% ± 31 (n = 4)

5.2 ± 1.3 (n = 5)

5.9 ± 2.1 (n = 4)

  1. Data are means obtained from multiple independent experiments (n), ±s.d.
  2. aMaximum AP activity observed relative to positive control, 500 pM E2
  3. bERα protein levels relative to vehicle control obtained by immunoblotting
  4. cInhibition of proliferation of MCF-7 cells stimulated with 100 pM E2 after 5–7 days
  5. dInhibition of an estrogen responsive reporter gene, ERE-tk109-Luc, transiently transfected into MCF-7 cells and stimulated with 100 pM E2 for 24 h
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