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Evotec Munich

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0,01<br />

0,1<br />

1<br />

10<br />

K d[µM]<br />

PAGE 12<br />

MAP4K5<br />

GAK<br />

ABL2<br />

ABL1<br />

LYN<br />

MAP4K3<br />

FYN<br />

SRC<br />

MAP4K4<br />

FRK<br />

CSK<br />

QIK<br />

EphA2<br />

EphB4<br />

MAP2K2<br />

ACK<br />

TNIK<br />

QSK<br />

SLK<br />

MAP2K1<br />

MAP3K2<br />

LOK<br />

YES<br />

MYT1<br />

ZAK<br />

EphB2<br />

FAK<br />

MAP3K4<br />

GCN2<br />

CK1d<br />

FER<br />

IKKe<br />

MST4<br />

MST3<br />

MST1<br />

SYK<br />

MAP2K6<br />

PYK2<br />

LRRK2<br />

ILK<br />

MST2<br />

TLK2<br />

Target profile of bosutinib in PC3 cells<br />

KinAffinity <br />

Native kinome profiling<br />

Bosutinib (SKI606, Wyeth) is currently tested in breast<br />

cancer and CML<br />

KinAffinity ® enriched nearly 200 endogenously expressed<br />

kinases from human prostate cancer (PC3) cells<br />

45 of these kinases were identified as molecular targets of<br />

bosutinib<br />

N<br />

O<br />

N O N<br />

Cl Cl<br />

HN O<br />

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