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Table 1 Kinase inhibition profile of ABT-869 (with permission adapted from Molecular Cancer Therapeutics 2006;5:995–1006)

From: ABT-869, a promising multi-targeted tyrosine kinase inhibitor: from bench to bedside

Related RTKa

Non-related TKa

Ser/Thr Kinasesb

Kinase

IC50 (nM)

Kinase

IC50 (nM)

Kinase

IC50 (nM)

KDR

8

SRC

> 50,000

AKT

> 50,000

FLT1

3

IGFR

> 50,000

SGK

940

FLT4

40

INSR

> 50,000

CDC2

9,800

PDGFRα

29

LCK

38,000

PKA

5,900

PDGFRβ

25

EGFR

> 50,000

  

CSF-1R

5

HCK

> 50,000

  

KIT

20

CMET

> 50,000

  

FLT3

10

LYN

> 20,000

  

TIE2

170

FYN

> 50,000

  

RET

1,900

FGR

> 50,000

  

FGFR

> 12,500

    
  1. a. IC50 values determined at an ATP concentration of 1 mM.
  2. b. IC50 values determined at an ATP concentration of 5 to 10 μM.