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Table 2 In vitro properties of SCR-6852

From: SCR-6852, an oral and highly brain-penetrating estrogen receptor degrader (SERD), effectively shrinks tumors both in intracranial and subcutaneous ER + breast cancer models

 

ERα degradation assay

Viability assay

 

DC50 nM

Dmax [% Ful.]

Dmax [% Veh.]

IC50 nM

Emax [% Ful.]

Emax [% Veh.]

MCF-7 WT

      

 Fulvestrant

0.93

97.69

56.04

0.40

97.88

49.60

 SCR-6852

1.05

100.45

57.61

0.72

96.22

48.96

 SCR-6515

0.08

97.83

66.81

0.29

103.00

64.15

 SCR-6139

0.31

101.13

69.02

0.40

98.77

58.83

MCF-7 Y537S

      

 Fulvestrant

32.05

87.09

26.38

16.29

95.49

65.05

 SCR-6852

47.32

99.57

30.17

27.6

100.96

68.78

MCF-8 D538G

      

 Fulvestrant

   

11.10

106.1

68.57

 SCR-6852

   

26.96

109.5

70.8

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Breast Cancer Research

ISSN: 1465-542X

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