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Table 1 HER2/neu and PI-9 status and cytotoxic effect of GrB, GrB-Fc-4D5 and Kadcyla on various tumor cell lines

From: Development of a human immuno-oncology therapeutic agent targeting HER2: targeted delivery of granzyme B

Cell Line

Cell Type

HER2/neua

PI-9b

IC50 (nM)

GrB

GrB-Fc-4D5

Kadcyla

Calu-3

Lung

109

0.5

> 1000

82

0.02

SKBR3

Breast

100

48

> 1000

56

0.02

NCI-N87

Gastric

85

8

> 1000

105

139

MDA-MB-453

Breast

13

0.4

532

32

0.55

SKOV3

Ovarian

11

100

> 1000

211

38

DU-145

Prostate

3.6

3

> 1000

45

152

MCF-7

Breast

3.4

38

> 1000

99

24

SKMEL28

Melanoma

3.4

73

> 1000

67

63

HT-29

Colon

3.0

0.6

> 1000

36

39

A-549

Lung

2.4

31

> 1000

55

78

MDA-MB-231

Breast

1.5

79

793

27

44

A375-M

Melanoma

1.5

27

> 1000

28

28

AAB-527

Melanoma

1.3

39

> 1000

57

25

MDA-MB-468

Breast

1.1

ND

> 1000

64

31

  1. Abbreviations: PI-9 serine protease inhibitor 9
  2. aHER2/neu receptor levels were determined by flow cytometry and normalized to the breast cancer cell line SKBR3
  3. bPI-9 protein levels were determined by Western blot analysis and normalized to the ovarian cancer cell line SKOV3