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Table 1 Kinase selectivity profiling of QAP 1 in radiometric filter binding assays

From: Catalytic inhibition of topoisomerase II by a novel rationally designed ATP-competitive purine analogue

Kinase

IC50 (μM)

Kinase

IC50 (μM)

HER-1

> 10

FGFR3-K560E

> 10

KDR

> 10

Axl

> 10

Flt-3

> 10

Fak

> 10

IGF-1R

> 10

c-Abl

> 10

Tek

> 10

c-Abl-T315I

> 10

c-Src

1.7 ± 0.5

PKA

> 10

c-Met

> 10

CDK1/CycB

> 10

Ret

1.35 ± 0.05

PKB

> 10

Jak2

> 10

PDK1

> 10

EphB4

> 10

BRAF-V600E

> 10

  1. QAP 1 was profiled against a panel of serine/threonine/tyrosine protein kinases. Data typically represent means of two independent experiments ± SD.