Table 1 Kinase selectivity profile of compounds.

From: DW14383 is an irreversible pan-FGFR inhibitor that suppresses FGFR-dependent tumor growth in vitro and in vivo

Kinase

IC50 (nmol/L)

DW14383

TAS-120

AZD4547

FGFR1

<0.3

3.9 ± 0.8

0.4 ± 0.1

FGFR2

1.1 ± 0.3

4.2 ± 0.0

1.0 ± 0.5

FGFR3

<0.3

8.1 ± 0.9

2.3 ± 0.2

FGFR4

0.5 ± 0.1

4.1 ± 1.2

49.8 ± 5.4

KDR

335.8 ± 25.2

>1000

57.9 ± 22.1

VEGFR-1

>100

>100

>100

PDGFR-α

>1000

>100

>1000

PDGFR-β

>100

>100

>1000

C-Kit

>100

>100

>100

Flt-3

>1000

>100

>1000

EGFR

>1000

>1000

>1000

ErbB2

>1000

>100

>1000

ErbB4

>100

>100

>1000

c-Src

>1000

>1000

>1000

ABL

>1000

>1000

>1000

EPH-A2

>1000

>1000

>1000

IGFIR

>100

>100

>1000

  1. aValues are the mean ± SD or estimated values of two or more independent assays.