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FGFR2 FGFR3<br />
TrkC<br />
EphB2<br />
TrkB<br />
FGFR1<br />
FGFR4<br />
EphB1<br />
TrkA<br />
FLT1/VEGFR1<br />
EphA5<br />
KDR/VEGFR2<br />
MuSK ROR2<br />
Fms/CSFR<br />
ROR1<br />
EphB3<br />
Ret<br />
Kit<br />
EphA3<br />
DDR2<br />
Mer<br />
EphA4<br />
DDR1<br />
Tyro3/<br />
Axl<br />
FLT4<br />
Sky<br />
PDGFRα<br />
EphA6<br />
IGF1R IRR<br />
FLT3<br />
PDGFRβ<br />
InsR<br />
Yes<br />
EphB4<br />
Met<br />
EGFR HER2/ErbB2<br />
Src<br />
Ron<br />
MLK3<br />
Ros<br />
EphA7<br />
ALK<br />
MLK1<br />
Lyn<br />
LTK<br />
Tie2<br />
Tie1<br />
HCK<br />
Fyn<br />
RYK<br />
HER4<br />
EphA8<br />
MLK4<br />
CCK4/PTK7<br />
MLK2<br />
Lck<br />
Fgr<br />
Ack Tnk1 Tyk2<br />
Jak1<br />
HER3<br />
Jak2<br />
EphA2<br />
Jak3<br />
BLK<br />
ANKRD3 SgK288<br />
DLK<br />
Syk Zap70/SRK<br />
EphA1<br />
PYK2/FAK2<br />
LZK<br />
FAK<br />
Lmr1<br />
ALK4<br />
ITK<br />
Lmr2<br />
C-Raf/Raf1<br />
FRK<br />
TGFβR1<br />
ZAK<br />
BRaf<br />
TEC<br />
EphB6<br />
KSR<br />
Srm<br />
RIPK2<br />
KSR2<br />
TXK<br />
Brk<br />
BTK<br />
Lmr3<br />
ALK7<br />
IRAK3<br />
IRAK1<br />
LIMK1<br />
ARaf<br />
BMPR1B<br />
Etk/BMX<br />
EphA10<br />
LIMK2 TESK1 ILK<br />
BMPR1A<br />
CTK<br />
RIPK3<br />
TSK2<br />
TAK1<br />
HH498<br />
ALK1<br />
CSK<br />
ALK2<br />
Abl2/Arg<br />
IRAK2<br />
ActR2<br />
Abl Fes<br />
ActR2B<br />
Fer<br />
RIPK1<br />
Jak3~b<br />
TGFβR2<br />
LRRK2<br />
MEKK2/MAP3K2<br />
Jak2~b<br />
LRRK1<br />
MISR2<br />
MEKK3/MAP3K3<br />
Tyk2~b<br />
SuRTK106<br />
IRAK4<br />
BMPR2<br />
ASK/MAP3K5<br />
ANPα/NPR1<br />
MAP3K8<br />
Jak1~b<br />
MAP3K7<br />
ANPβ/NPR2<br />
KHS1<br />
MOS<br />
KHS2<br />
HSER<br />
SgK496<br />
WNK1<br />
WNK3<br />
MEKK6/MAP3K6<br />
DYRK2<br />
Mst4<br />
PBK<br />
MAP3K4<br />
DYRK3<br />
GUCY2D<br />
WNK2<br />
DYRK4<br />
DYRK1A<br />
GUCY2F<br />
OSR1<br />
DYRK1B<br />
WNK4<br />
MLKL<br />
PERK/PEK<br />
SgK307<br />
SLK<br />
PKR<br />
LOK<br />
HIPK1 HIPK3<br />
GCN2 SgK424<br />
TAO1<br />
SCYL3 TAO2<br />
HIPK2<br />
SCYL1<br />
Tpl2/COT<br />
SCYL2<br />
NIK<br />
TAO3<br />
PAK1<br />
HIPK4<br />
PRP4<br />
HRI<br />
PAK3 PAK4<br />
CLIK1<br />
PAK2<br />
IRE1<br />
MAP2K5<br />
PAK5/PAK7<br />
CLIK1L<br />
IRE2<br />
CLK3<br />
TBCK<br />
PAK6<br />
MAP2K7<br />
MEK1/MAP2K1<br />
RNAseL<br />
GCN2~b<br />
MEK2/MAP2K2<br />
TTK<br />
MSSK1<br />
SgK071<br />
SRPK2<br />
KIS<br />
MYT1<br />
SEK1/MAP2K4 MKK3/MKK6<br />
SRPK1<br />
CK2α1<br />
Wee1<br />
MAK<br />
CK2α2<br />
SgK196<br />
CDC7<br />
Wee1B<br />
CK1δ<br />
ICK<br />
PRPK<br />
TTBK1<br />
CK1ε<br />
GSK3β<br />
MOK<br />
TTBK2<br />
GSK3α<br />
CK1α1<br />
CDKL3<br />
CK1α2<br />
CDKL2<br />
PINK1<br />
SgK493<br />
SgK269<br />
VRK3<br />
CK1γ2<br />
CDKL1 CDKL5<br />
ERK7<br />
SgK396<br />
SgK223<br />
CDKL4 Erk4<br />
Slob<br />
CK1γ1<br />
Erk3<br />
SgK110<br />
PIK3R4<br />
CK1γ3<br />
NLK<br />
SgK069<br />
Bub1<br />
Erk5<br />
SBK<br />
BubR1<br />
Erk1/<br />
IKKα<br />
p44MAPK<br />
IKKβ<br />
VRK1<br />
CDK7<br />
IKKε<br />
VRK2<br />
Erk2/<br />
PLK4<br />
PITSLRE<br />
TBK1/NAK<br />
p42MAPK p38γ<br />
MPSK1<br />
JNK1<br />
p38δ<br />
JNK2<br />
TLK2<br />
JNK3 CDK10<br />
GAK<br />
TLK1<br />
PLK3<br />
p38β<br />
AAK1<br />
CAMKK1<br />
ULK3<br />
PLK1<br />
p38α<br />
PLK2<br />
CDK4<br />
CCRK<br />
BIKE<br />
CAMKK2<br />
BARK1/GRK2<br />
CDK6<br />
ULK1<br />
BARK2/GRK3 RHOK/GRK1<br />
Fused<br />
GRK5<br />
PFTAIRE2<br />
SgK494<br />
ULK2 ULK4<br />
GRK6 GRK4<br />
PFTAIRE1<br />
CDK9<br />
Nek6<br />
RSKL1<br />
PCTAIRE2<br />
Nek7 Nek10<br />
SgK495<br />
PASK<br />
PDK1<br />
RSKL2<br />
Nek8<br />
MSK1<br />
RSK1/p90RSK<br />
PCTAIRE1<br />
CDK5 CRK7<br />
PCTAIRE3<br />
Nek9<br />
LKB1<br />
MSK2<br />
RSK4 RSK2<br />
Chk1<br />
p70S6K<br />
RSK3<br />
Nek2<br />
Akt2/PKBβ<br />
AurA/Aur2<br />
p70S6Kβ<br />
Akt1/PKBα<br />
cdc2/CDK1<br />
Nek11<br />
Akt3/PKBγ<br />
CDK3<br />
Nek4<br />
AurB/Aur1<br />
SGK1<br />
CDK2<br />
AurC/Aur3<br />
SGK2<br />
SGK3<br />
Trb3 Pim1 Pim2<br />
PKG2<br />
PKN1/PRK1<br />
LATS1<br />
Nek3<br />
PKG1<br />
PKN2/PRK2<br />
Trb2<br />
Pim3<br />
LATS2<br />
PKN3<br />
Nek5<br />
NDR1<br />
PRKY<br />
PKCδ<br />
Trb1<br />
Obscn~b<br />
NDR2<br />
PKCθ<br />
PRKX<br />
YANK1<br />
SPEG~b<br />
MAST3<br />
PKCη<br />
Nek1<br />
MASTL<br />
PKCε<br />
Obscn<br />
STK33<br />
YANK2<br />
PKCι<br />
YANK3<br />
PKCζ<br />
SPEG<br />
PKAγ<br />
PKAα<br />
PKCγ<br />
TTN<br />
MAST2<br />
PKAβ<br />
smMLCK<br />
TSSK4<br />
ROCK1<br />
PKCα<br />
HUNK<br />
ROCK2<br />
Chk2/Rad53<br />
PKCβ<br />
skMLCK<br />
SSTK<br />
SNRK<br />
MAST4 MAST1<br />
DMPK<br />
NIM1<br />
CRIK<br />
DRAK1 TSSK3<br />
PKD2/PKCμ<br />
TSSK1<br />
SgK085<br />
TSSK2<br />
DMPK2<br />
caMLCK<br />
PKD1<br />
DCAMKL3<br />
DAPK2<br />
DAPK3<br />
DCAMKL1<br />
MELK PKD3/PKCν<br />
DAPK1<br />
DCAMKL2<br />
MRCKβ<br />
VACAMKL<br />
MRCKα<br />
MNK1<br />
PhKγ1<br />
MNK2<br />
PhKγ2<br />
PSKH1<br />
CaMKIIγ<br />
PSKH2<br />
BRSK2<br />
CaMKIIα<br />
CaMKIIβ<br />
BRSK1<br />
CaMKIIδ<br />
RSK4~b<br />
SNARK<br />
RSK1~b<br />
CaMKIV<br />
ARK5<br />
MSK2~b<br />
MSK1~b<br />
QSK<br />
RSK3~b<br />
RSK2~b<br />
CaMKIβ<br />
SIK<br />
QIK<br />
CaMKIγ<br />
MARK4<br />
CaMKIα<br />
CaMKIδ<br />
MARK3<br />
CHED<br />
DRAK2<br />
AMPKα2<br />
AMPKα1<br />
Haspin<br />
CASK<br />
MAPKAPK5<br />
MAPKAPK2<br />
MAPKAPK3<br />
STLK3<br />
STRAD/STLK5<br />
STLK6<br />
GRK7<br />
HPK1<br />
GCK<br />
NRK/ZC4<br />
Mst1<br />
Mst2<br />
TNIK/ZC2<br />
MYO3A<br />
MYO3B<br />
YSK1<br />
Mst3<br />
HGK/ZC1<br />
MINK/ZC3<br />
Section I: Research Areas<br />
chapter 02: Signaling<br />
Tyrosine Kinases and<br />
Associated Phosphatases<br />
Tyrosine Kinase Signaling<br />
Whether functioning as cell surface receptors or as internal effectors of cell signaling, tyosine kinases<br />
control multiple aspects of cell and organism growth, differentiation, and function. Approximately 20<br />
receptor tyrosine kinase (RTK) families and at least 9 distinct groups of nonreceptor tyrosine kinases<br />
have been identified in humans. Regardless of localization, all tyrosine kinases regulate target protein<br />
function through transfer of phosphate from ATP to the hydroxyl group of a target protein tyrosine.<br />
EGF stimulation results in<br />
phosphorylation of EGFR at Tyr1068.<br />
Phospho-EGF Receptor (Tyr1068) (D7A5) XP ® Rabbit mAb #3777:<br />
WB analysis of extracts of BxPC-3 cells, untreated or EGF-stimulated,<br />
using #3777 (upper) and EGF Receptor Antibody #2232 (lower).<br />
kDa<br />
200<br />
140<br />
100<br />
80<br />
200<br />
140<br />
100<br />
80<br />
+<br />
–<br />
Phospho-<br />
EGFR<br />
(Tyr1068)<br />
EGFR<br />
EGF<br />
The tyrosine kinase family, a distinct<br />
group within the human kinome<br />
CMGC<br />
CLK4<br />
CLK2 CLK1<br />
TK<br />
CDK8 CDK11<br />
MARK1<br />
MARK2<br />
Receptor Tyrosine Kinases<br />
Most RTKs are single-pass, transmembrane<br />
proteins that bind extracellular polypeptide ligands<br />
(i.e. growth factors) and cytoplasmic effector and<br />
adaptor proteins to regulate biological processes.<br />
Ligand binding promotes receptor dimerization and<br />
autophosphorylation of receptor tyrosine residues.<br />
The resultant conformational change stabilizes the<br />
active kinase, and subsequent phosphorylation<br />
events form binding sites for downstream adaptor,<br />
scaffold, and effector proteins.<br />
EGFR phosphorylation at multiple<br />
tyrosine residues provides binding<br />
sites for adaptor proteins and<br />
downstream signaling nodes.<br />
Trad Trio<br />
CAMK<br />
FGFR2 FGFR3<br />
TrkC<br />
EphB2<br />
TrkB<br />
FGFR1<br />
FGFR4<br />
EphB1<br />
TrkA<br />
FLT1/VEGFR1<br />
EphA5<br />
KDR/VEGFR2<br />
MuSK ROR2<br />
Fms/CSFR<br />
ROR1<br />
EphB3<br />
Ret<br />
Kit<br />
EphA3<br />
DDR2<br />
Mer<br />
EphA4<br />
DDR1<br />
Tyro3/<br />
Axl<br />
FLT4<br />
Sky<br />
PDGFRα<br />
EphA6<br />
IGF1R IRR<br />
FLT3<br />
PDGFRβ<br />
InsR<br />
Yes<br />
EphB4<br />
Met<br />
EGFR HER2/ErbB2<br />
Src<br />
Ron<br />
MLK3<br />
Ros<br />
EphA7<br />
ALK<br />
MLK1<br />
Lyn<br />
LTK<br />
Tie2<br />
Tie1<br />
HCK<br />
Fyn<br />
RYK<br />
HER4<br />
EphA8<br />
MLK4<br />
CCK4/PTK7<br />
MLK2<br />
Lck<br />
Fgr<br />
Ack Tnk1 Tyk2<br />
Jak1<br />
HER3<br />
Jak2<br />
EphA2<br />
Jak3<br />
BLK<br />
TKL<br />
ANKRD3 SgK288<br />
DLK<br />
Syk Zap70/SRK<br />
EphA1<br />
PYK2/FAK2<br />
LZK<br />
TKL<br />
FAK<br />
Lmr1<br />
ALK4<br />
ITK<br />
Lmr2<br />
C-Raf/Raf1<br />
FRK<br />
TGFβR1<br />
ZAK<br />
BRaf<br />
TEC<br />
EphB6<br />
KSR<br />
Srm<br />
RIPK2<br />
KSR2<br />
TXK<br />
Brk<br />
BTK<br />
Lmr3<br />
ALK7<br />
IRAK3<br />
IRAK1<br />
LIMK1<br />
ARaf<br />
BMPR1B<br />
Etk/BMX<br />
EphA10<br />
LIMK2 TESK1 ILK<br />
BMPR1A<br />
CTK<br />
RIPK3<br />
TSK2<br />
TAK1<br />
HH498<br />
ALK1<br />
CSK<br />
ALK2<br />
Abl2/Arg<br />
IRAK2<br />
ActR2<br />
Abl Fes<br />
ActR2B<br />
Fer<br />
RIPK1<br />
Jak3~b<br />
TGFβR2<br />
LRRK2<br />
MEKK2/MAP3K2<br />
Jak2~b<br />
LRRK1<br />
MISR2<br />
MEKK3/MAP3K3<br />
Tyk2~b<br />
SuRTK106<br />
IRAK4<br />
BMPR2<br />
ASK/MAP3K5<br />
ANPα/NPR1<br />
MAP3K8<br />
Jak1~b<br />
MAP3K7<br />
ANPβ/NPR2<br />
NRBP1 NRBP2 MEKK1/MAP3K1<br />
KHS1<br />
MOS<br />
KHS2<br />
HSER<br />
SgK496<br />
WNK1<br />
STE<br />
WNK3<br />
MEKK6/MAP3K6<br />
DYRK2<br />
Mst4<br />
PBK<br />
MAP3K4<br />
DYRK3<br />
GUCY2D<br />
WNK2<br />
DYRK4<br />
DYRK1A<br />
NRBP1<br />
GUCY2F<br />
NRBP2 MEKK1/MAP3K1 OSR1<br />
DYRK1B<br />
WNK4<br />
MLKL<br />
PERK/PEK<br />
SgK307<br />
SLK<br />
PKR<br />
LOK<br />
HIPK1 HIPK3<br />
GCN2 SgK424<br />
TAO1<br />
SCYL3 TAO2<br />
HIPK2<br />
SCYL1<br />
Tpl2/COT<br />
SCYL2<br />
NIK<br />
TAO3<br />
PAK1<br />
CLK4 HIPK4<br />
PRP4<br />
HRI<br />
PAK3<br />
CLIK1<br />
PAK2<br />
IRE1<br />
CLK2 CLK1<br />
PAK4<br />
MAP2K5<br />
PAK5/PAK7<br />
CLIK1L<br />
IRE2<br />
CLK3<br />
TBCK<br />
PAK6<br />
MAP2K7<br />
MEK1/MAP2K1<br />
RNAseL<br />
GCN2~b<br />
MEK2/MAP2K2<br />
CK1<br />
TTK<br />
MSSK1<br />
SgK071<br />
SRPK2<br />
KIS<br />
MYT1<br />
SEK1/MAP2K4 MKK3/MKK6<br />
SRPK1<br />
CK2α1<br />
Wee1<br />
MAK<br />
CK2α2<br />
SgK196<br />
CDC7<br />
Wee1B<br />
CK1δ<br />
ICK<br />
PRPK<br />
TTBK1<br />
CK1ε<br />
GSK3β<br />
AGC<br />
MOK<br />
TTBK2<br />
GSK3α<br />
CK1α1<br />
CDKL3<br />
CK1α2<br />
CDKL2<br />
PINK1<br />
SgK493<br />
SgK269<br />
VRK3<br />
CK1γ2<br />
CDKL1 CDKL5<br />
ERK7<br />
SgK396<br />
SgK223<br />
CDKL4 Erk4<br />
Slob<br />
CK1γ1<br />
Erk3<br />
SgK110<br />
PIK3R4<br />
CK1γ3<br />
NLK<br />
SgK069<br />
Bub1<br />
Erk5<br />
SBK<br />
BubR1<br />
Erk1/<br />
IKKα<br />
p44MAPK<br />
IKKβ<br />
VRK1<br />
CDK7<br />
IKKε<br />
VRK2<br />
Erk2/<br />
PLK4 CK1<br />
PITSLRE<br />
TBK1/NAK<br />
p42MAPK p38γ<br />
MPSK1<br />
JNK1<br />
p38δ<br />
JNK2<br />
TLK2<br />
JNK3 CDK10<br />
GAK<br />
TLK1<br />
PLK3<br />
p38β<br />
AAK1<br />
CDK8 CDK11<br />
CAMKK1<br />
ULK3<br />
PLK1<br />
p38α<br />
PLK2<br />
CDK4<br />
CCRK<br />
BIKE<br />
CAMKK2<br />
BARK1/GRK2<br />
CDK6<br />
CMGC<br />
ULK1<br />
BARK2/GRK3 RHOK/GRK1<br />
Fused<br />
GRK5<br />
PFTAIRE2<br />
SgK494<br />
ULK2 ULK4<br />
GRK6 GRK4<br />
PFTAIRE1<br />
CDK9<br />
Nek6<br />
RSKL1<br />
PCTAIRE2<br />
Nek7 Nek10<br />
SgK495<br />
PASK<br />
PDK1<br />
RSKL2<br />
Nek8<br />
MSK1<br />
RSK1/p90RSK<br />
PCTAIRE1<br />
CDK5 CRK7<br />
PCTAIRE3<br />
Nek9<br />
LKB1<br />
MSK2<br />
RSK4 RSK2<br />
Chk1<br />
p70S6K<br />
RSK3<br />
Nek2<br />
Akt2/PKBβ<br />
AurA/Aur2<br />
p70S6Kβ<br />
Akt1/PKBα<br />
cdc2/CDK1<br />
Nek11<br />
Akt3/PKBγ<br />
CDK3<br />
Nek4<br />
AurB/Aur1<br />
SGK1<br />
CDK2<br />
AurC/Aur3<br />
SGK2<br />
SGK3<br />
Trb3 Pim1 Pim2<br />
PKG2<br />
PKN1/PRK1<br />
LATS1<br />
Nek3<br />
PKG1<br />
PKN2/PRK2<br />
Trb2<br />
Pim3<br />
PKN3<br />
Nek5<br />
Trad Trio<br />
LATS2<br />
NDR1<br />
PRKY<br />
PKCδ<br />
Trb1<br />
Obscn~b<br />
NDR2<br />
PKCθ<br />
PRKX<br />
YANK1<br />
SPEG~b<br />
MAST3<br />
PKCη<br />
Nek1<br />
MASTL<br />
PKCε<br />
Obscn<br />
STK33<br />
YANK2<br />
PKCι<br />
YANK3<br />
PKCζ<br />
SPEG<br />
PKAγ<br />
PKAα<br />
PKCγ<br />
TTN<br />
MAST2<br />
PKAβ<br />
smMLCK<br />
TSSK4<br />
ROCK1<br />
PKCα<br />
HUNK<br />
ROCK2<br />
Chk2/Rad53<br />
PKCβ<br />
skMLCK<br />
SSTK<br />
SNRK<br />
MAST4 MAST1<br />
DMPK<br />
NIM1<br />
CRIK<br />
DRAK1 TSSK3<br />
PKD2/PKCμ<br />
TSSK1<br />
SgK085<br />
TSSK2<br />
DMPK2<br />
EGF<br />
caMLCK<br />
PKD1<br />
DCAMKL3<br />
DAPK2<br />
DAPK3<br />
DCAMKL1<br />
MELK PKD3/PKCν<br />
DAPK1<br />
DCAMKL2<br />
MRCKβ<br />
VACAMKL<br />
MRCKα<br />
MNK1<br />
PhKγ1<br />
MNK2<br />
PhKγ2<br />
PSKH1<br />
CaMKIIγ<br />
PSKH2<br />
BRSK2<br />
CaMKIIα<br />
CaMKIIβ<br />
NH 2<br />
BRSK1<br />
CaMKIIδ<br />
RSK4~b<br />
SNARK<br />
RSK1~b<br />
CaMKIV<br />
ARK5<br />
MSK2~b<br />
MSK1~b<br />
CaMKII<br />
CaMKII<br />
Cys<br />
rich<br />
CHED<br />
Tyr845<br />
Tyr974<br />
Tyr992<br />
Tyr1045<br />
Ser1046<br />
Ser1047<br />
Ser1057<br />
Tyr1068<br />
Tyr1086<br />
Tyr1101<br />
Ser1142<br />
Tyr1148<br />
Tyr1173<br />
TK<br />
Src phosphorylation<br />
Autophosphorylation<br />
kinase domain<br />
kinase domain<br />
COOH<br />
EGFR homodimer<br />
P<br />
P<br />
P<br />
P<br />
P<br />
P<br />
P<br />
P<br />
P<br />
P<br />
P<br />
P<br />
P<br />
STAT5b<br />
AP-2<br />
PLCγ<br />
Cbl<br />
ubiquitination<br />
Grb2<br />
Gab1<br />
ubiquitination<br />
SHC<br />
SHP1<br />
PLCγ<br />
DRAK2<br />
CAMK<br />
DNA synthesis<br />
Translocation to<br />
mitochondria survival<br />
PKC<br />
ubiquitination<br />
p85<br />
PKC<br />
AMPKα2<br />
AMPKα1<br />
QSK<br />
SIK<br />
QIK<br />
degradation<br />
degradation<br />
MARK4<br />
MARK3<br />
MARK1<br />
MARK2<br />
MAPK/ERK<br />
Cascade<br />
degradation<br />
MAPK/ERK<br />
Cascade<br />
AKT/PKB<br />
Cascade<br />
MAPK/ERK<br />
Cascade<br />
Haspin<br />
RSK3~b<br />
RSK2~b<br />
CASK<br />
MAPKAPK5<br />
MAPKAPK2<br />
MAPKAPK3<br />
STLK3<br />
STRAD/STLK5<br />
STLK6<br />
CaMKIβ<br />
CaMKIγ<br />
CaMKIα<br />
CaMKIδ<br />
GRK7<br />
HPK1<br />
GCK<br />
NRK/ZC4<br />
Mst1<br />
Mst2<br />
TNIK/ZC2<br />
MYO3A<br />
MYO3B<br />
YSK1<br />
Mst3<br />
RTKs regulate a broad range of biological effects including cell growth, proliferation, survival, migration,<br />
STE and differentiation. For this reason, altered levels and/or activities of RTKs are commonly associated<br />
with many forms of human cancer. RTK activity can be chemically manipulated through the use of<br />
targeted, small-molecule inhibitors.<br />
HGK/ZC1<br />
MINK/ZC3<br />
Phospho-EGF Receptor (Tyr1068) (D7A5)<br />
XP ® Rabbit mAb #3777: Confocal IF analysis<br />
of HeLa cells, untreated (left) or EGF-treated<br />
(right), using #3777 (green). Blue pseudocolor<br />
= DRAQ5 ® #4084 (fluorescent DNA dye).<br />
HER2, an ErbB/HER family member, is<br />
overexpressed in 40% of human breast cancers.<br />
AGC<br />
HER2/ErbB2 (D8F12) XP ® Rabbit mAb #4290: IHC analysis of paraffin-embedded<br />
human breast carcinoma using #4290.<br />
ROS1, an RTK similar in structure to ALK that<br />
forms oncogenic fusion proteins with FIG1,<br />
SLC34A2, and CD74<br />
ROS1 (D4D6 ® ) Rabbit mAb #3287: IHC analysis of paraffin-embedded human lung<br />
carcinoma using #3287. Note: Staining is of FIG-ROS1 fusion.<br />
HER3/ErbB3 is overexpressed in many forms<br />
of cancer.<br />
HER3/ErbB3 (D22C5) XP ® Rabbit mAb #12708: IHC analysis of paraffin-embedded<br />
non-small cell lung carcinoma using #12708.<br />
Ligand activation<br />
of EGFR at the cell<br />
membrane results<br />
in phosphorylation<br />
at Tyr1068.<br />
Tyrosine Kinase<br />
Inhibitors<br />
#4401 Crizotinib<br />
Inhibitor of ALK and ROS1<br />
(ATP-competitive inhibitor)<br />
#9052 Dasatinib<br />
Tyrosine kinase inhibitor<br />
(Abl, BCR/Abl, Src, c-KIT,<br />
Ephrin receptors)<br />
#5083 Erlotinib<br />
Inhibits EGFR<br />
(ATP-competitive inhibitor)<br />
#4765 Gefitinib<br />
Inhibits EGFR<br />
(active site inhibitor)<br />
#9084 Imatinib<br />
Inhibits Bcr-Abl, PDGFR,<br />
c-Kit (active site inhibitor)<br />
#12121 Lapatinib<br />
Inhibits EGFR and HER2<br />
(ATP-competitive inhibitor)<br />
#12209 Nilotinib<br />
Tyrosine kinase inhibitor<br />
(Abl, BCR/Abl, c-KIT, LCK,<br />
Ephrin receptors, DDR1/2,<br />
PDGFR-B)<br />
#9493 PKC412<br />
Very broad spectrum protein<br />
kinase inhibitor (conventional<br />
PKCs, some RTKs, Syk,<br />
Cdk1/B, c-Src)<br />
#8705 Sorafenib<br />
Inhibits VEGFR and PDGFR;<br />
inhibits Raf kinases; Induces<br />
autophagy<br />
#12328 Sunitinib<br />
Broad RTK inhibitor<br />
(PDGFR, VEGFR, c-KIT, RET,<br />
CSF-1R, FLT-3/CD135)<br />
#9842 Tyrphostin AG 1478<br />
Inhibits EGFR<br />
#12998 Vatalanib<br />
Broad RTK inhibitor<br />
(VEGFR, PDGFR-B, c-KIT)<br />
66 For Research Use Only. Not For Use in Diagnostic Procedures. See pages 302 & 303 for Pathway Diagrams, Application, and Reactivity keys.<br />
www.cellsignal.com/csttyrosine<br />
67
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