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Table 1 Inhibitors identified in the kinase inhibitor screen

From: Aurora kinase B is important for antiestrogen resistant cell growth and a potential biomarker for tamoxifen resistant breast cancer

Inhibitor

Inhibitory Effect ± SD (%)

Target(s)

T47D

182R-1

182R-2

Barasertib

28.2 ± 1.7

58.9 ± 2.2

59.9 ± 2.1

Aurora B

PHA-680632

23.5 ± 7.4

62.8 ± 2.7

56.1 ± 5.0

Aurora A/B/C

SNS-314 Mesylate

19.4 ± 1.5

47.0 ± 2.6

52.8 ± 5.1

Aurora A/B/C

ZM-447439

24.2 ± 6.1

57.7 ± 1.8

65.6 ± 1.5

Aurora A/B/C

CCT129202

20.1 ± 13.2

44.5 ± 4.8

48.8 ± 4.3

Aurora A/B/C

AMG 900

25.3 ± 3.0

55.8 ± 4.5

55.5 ± 0.6

Aurora A/B/C

JNJ-7706621

1.7 ± 5.7

27.5 ± 4.9

33.4 ± 4.8

Aurora A/B, cyclin A/CDK2, cyclin E/CDK2, cyclin B/CDK1

AT9283

6.2 ± 3.6

46.4 ± 2.5

52.6 ± 2.1

Aurora A/B, JAK2/3 and Abl

ENMD-2076

24.3 ± 16.5

61.8 ± 2.8

65.7 ± 1.5

Aurora A/B, Flt3/4, SFKs and VEGFR2

AZD7762

8.6 ± 10.3

30.3 ± 1.1

33.8 ± 2.8

Chk1/2

CX-4945

8.2 ± 2.1

27.9 ± 1.7

21.8 ± 1.7

CK2

PF-562271

1.4 ± 4.5

19.0 ± 3.5

14.8 ± 2.5

FAK and Pyk2

Nintedanib

11.8 ± 3.0

42.2 ± 3.5

33.9 ± 6.2

FGFR, VEGFR, PDGRF and SFKs

Dasatinib

18.0 ± 3.5

47.1 ± 2.7

37.0 ± 3.4

SFKs, Abl and c-Kit

TG100-115

5.0 ± 1.5

12.9 ± 2.3

13.2 ± 5.3

PI3Kγ/δ

  1. The growth inhibitory effect of the kinase inhibitors compared with untreated cells ± standard deviation (SD). Abbreviations: Abelson (Abl), Casein kinase (CK), checkpoint kinase (Chk), cyclin-dependent kinases (CDK), fibroblast growth factor receptor (FGFR), Fms-like Tyrosine Kinase (Flt), focal adhesion kinase (FAK), janus kinase (JAK), platelet-derived growth factor receptor (PDGFR), proline-rich tyrosine kinase (Pyk), Src Family kinases (SFKs), vascular endothelial growth factor receptor (VEGFR), and phosphoinositide 3-kinase (PI3K).