Transcript Slide 1

Figure S1, FGFR2 copy gain and overexpression in H716 cells
A
NCI H716 colon adenocarcinoma
View Key
FGFR2 (MB 122)
B
KATOIII gastric cancer
FGFR2 (MB 122)
C
Figure S1C: Selective FGFR2 overexpression in H716, KATOIII and SNU16 cell
lines in Wooster Cell Line
Reporter:
KatoIII
SNU16
H716
18,823 measured genes
10-123287897
338 samples
Figure S2: FGF2 does not further activate FGFR2 in H716 or colon cancer cell lines.
SW620
-
SW48
+
+
RKO
SW480
-
-
+
H747
DLD1
+
-
+
LS411N
-
-
+
-
+
-
+
-
FGF2
H508
+
H716
FGFR2
-150
p-FGFR2
-150
Actin
- 40
80-100%activity :
Kinase
% Control
FGFR1
FGFR3
FGFR2
DDR1
MKNK1
FLT4
PIK3CB
CSF1R
NEK4
NEK11
FGFR4
STK25
STK24
CHUK
NUAK1
MAPK13
MAP2K4
NTRK2
MATK
ERBB3
ABL1
RIOK2
AKT1
BTK
DCLK1
CDK4
PIK3CA
HIPK2
EGFR
MAP2K6
RPS6KA4
NUAK2
FLT3
HUNK
MAPK9
STK3
KDR
DYRK2
LCK
MAP3K3
TAOK3
TRPM6
CDKL3
EIF2AK2
TSSK1B
MAP3K2
PDGFRB
PLK1
1.4
1.6
2.4
18
34
35
35
36
54
55
56
57
58
62
67
67
68
68
69
69
70
71
72
72
72
73
73
74
76
76
76
76
77
77
77
77
77
78
78
78
78
78
79
79
79
80
80
80
AAK1
ABL1
ABL2
ACVR1
ACVR1B
ACVR2A
ACVR2B
ACVRL1
ADCK4
AKT2
AKT3
ALK
ANKK1
AURKA
AURKB
AURKC
AXL
BLK
BMP2K
BMPR1A
BMPR1B
BMPR2
BMX
BRAF
BRSK1
BRSK2
CABC1
CAMK1
CAMK1D
CAMK1G
CAMK2A
CAMK2B
CAMK2D
CAMK2G
CAMK4
CAMKK1
CAMKK2
CASK
CDC2L1
CDC2L2
CDC2L5
CDC2L6
CDC42BPA
CDC42BPB
CDC42BPG
Figure S3: AMBIT panel with 100nM PD173074
CDK2
CDK3
CDK4
CDK5
CDK7
CDK8
CDK9
CDKL1
CDKL2
CDKL5
CHEK1
CHEK2
CIT
CLK1
CLK2
CLK3
CLK4
CSK
CSNK1A1
CSNK1A1L
CSNK1D
CSNK1E
CSNK1G1
CSNK1G2
CSNK1G3
CSNK2A1
CSNK2A2
DAPK1
DAPK2
DAPK3
DCLK2
DCLK3
DDR2
DMPK
DSTKY
DYRK1A
DYRK1B
EGFR
EIF2AK1
EIF2AK4
EPHA1
EPHA2
EPHA3
EPHA4
EPHA5
EPHA6
EPHA7
EPHA8
EPHB1
EPHB2
EPHB3
EPHB4
EPHB6
ERBB2
ERBB4
ERN1
FER
FES
FGR
FLT1
FLT3
FRAP1
FRK
FYN
GAK
GRK1
GRK4
GRK7
GSK3A
GSK3B
HCK
HIPK1
HIPK3
HIPK4
ICK
IGF1R
IKBKB
IKBKE
INSR
INSRR
IRAK1
IRAK3
IRAK4
ITK
JAK1
JAK1
JAK2
JAK3
KIAA0999
KIT
LATS1
LATS2
LIMK1
LIMK2
LRRK2
LRRK2
LTK
LYN
MAK
MAL13P1.279
MAP2K1
MAP2K2
MAP2K3
MAP2K5
MAP2K7
MAP3K1
MAP3K10
MAP3K11
MAP3K12
MAP3K13
MAP3K15
MAP3K2
MAP3K4
MAP3K5
MAP3K6
MAP3K7
MAP3K9
MAP4K1
MAP4K2
MAP4K3
MAP4K4
MAP4K5
MAPK1
MAPK10
MAPK11
MAPK12
MAPK14
MAPK15
MAPK3
MAPK4
MAPK6
MAPK7
MAPK8
MAPKAPK2
MAPKAPK5
MARK1
MARK2
MARK3
MARK4
MAST1
MELK
MERTK
MET
MGC42105
MINK1
MKNK2
MST1R
MST4
MUSK
MYLK
MYLK2
MYLK3
MYLK4
MYO3A
MYO3B
NEK1
NEK2
NEK3
NEK5
NEK6
NEK7
NEK9
NLK
NTRK1
NTRK3
OXSR1
PAK1
PAK2
PAK3
PAK4
PAK6
PAK7
PCTK1
PCTK2
PCTK3
PDGFRA
PDGFRB
PDPK1
PFB0815w
PFTK1
PFTK2
PHKG1
PHKG2
PI4KB
PIK3C2B
PIK3C2G
PIK3CA
PIK3CD
PIK3CG
PIM1
PIM2
PIM3
PIP4K2B
PIP4K2C
PIP5K1A
PIP5K1C
PKMYT1
PKN1
PKN2
pknB
PLK1
PLK2
PLK3
PLK4
PRKAA1
PRKAA2
PRKACA
PRKACB
PRKCD
PRKCE
PRKCH
PRKCI
PRKCQ
PRKD1
PRKD2
PRKD3
PRKG1
PRKG2
PRKX
PRPF4B
PTK2
PTK2B
PTK6
RAF1
RET
RIOK1
RIOK3
RIPK1
RIPK2
RIPK4
ROCK1
ROCK2
ROS1
RPS6KA1
RPS6KA1
RPS6KA2
RPS6KA2
RPS6KA3
RPS6KA4
RPS6KA5
RPS6KA5
RPS6KA6
RPS6KA6
RPS6KB1
SBK1
SgK110
SGK3
SIK1
SIK2
SLK
SNRK
SRC
SRMS
SRPK1
SRPK2
SRPK3
STK10
STK11
STK16
STK17A
STK17B
STK32A
STK32B
STK32C
STK33
STK35
STK36
STK38
STK38L
STK39
STK4
SYK
TAOK1
TAOK2
TBK1
TEC
TEK
TESK1
TGFBR1
TGFBR2
TIE1
TLK1
TLK2
TNIK
TNK1
TNK2
TNNI3K
TTK
TXK
TYK2
TYK2
TYRO3
ULK1
ULK2
ULK3
VRK2
WEE1
WEE2
YES1
YSK4
ZAK
ZAP70
Figure S4:
PD173074 Inhibits pFGFR2 and selectively inhibits NCI-H716 growth
B
A
IC50
100
80
60
40
20
0
T = 3 days
Figure S5: pRSK S359/363 (ERK phosphorylation site) is inhibited by PD173074
PD173074 : P-359/363 RSK
+
-100
-75
GAPDH
Figure S6: L-547 and Rapamycin inhibit Akt and S6RP phosphorylation
B
A
1uM L547
pAkt
Akt
:
-
+
Rapamycin
-60
pS6RP
+
-35
-60
S6RP
GAPDH
-
-35
-35
-35
GAPDH
Figure S7: PD173074 causes cell
death in NCI-H716 cells
.
Untreated
PD173074 100nM
Figure S8: E cadherin and EPCAM are not expressed in H716 cells
SW620
-
SW48
+
+
-
RKO
SW480
-
+
H747
DLD1
+
-
+
LS411N
-
-
+
-
+
-
+
-
H80
H508
+
H716
FGF2
-150
CDH1
-- 120
EPCAM
-30
Actin
-40