Table 4 In-vitro selectivity of compound 13a and 13k.

From: Rational Design, Synthesis and Biological Evaluation of Pyrimidine-4,6-diamine derivatives as Type-II inhibitors of FLT3 Selective Against c-KIT

Kinase

aIC50 (nM) ± SD

13a

13k

FLT3

13.93 ± 6.5

63.02 ± 12

FLT3D835Y

72.52 ± 14.4

13713 ± 234

c-KIT

8,799 ± 2,083

/

CSF-1R

13,040 ± 231

60.7% at 20 µM

RET

4710 ± 342

1,664

RETV804L

62.3% at 20 µM

40.8% at 20 µM

Aurora B

79.8% at 20 µM

71.9% at 20 µM

  1. aIC50 values are expressed in nM units and are the results of three independent experiments.
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