导图社区 FGFR screening cascade
FGFR screening cascade from ICE Bioscence:Selectivity and MOA Study:pFGFR3 functional whole blood HTRF assay。
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FGFR3 screening
Screening
Primary Screen
FGFR TR-FRET biochemical assay
FGFR1-3 wt and mutant
FGFR4
Proliferation assay
RT-112 (FGFR3-TACC3)
RT-112/84 (FGFR3-TACC3)
RT-112-V555M (FGFR3-TACC3 V555M)
Secondary Screen
UM-UC-14 (FGFR3 S249C)
RT-4(FGFR3-TACC3)
pFGFR2 phosphorylation
HTRF assay
KATO-III (FGFR2 amplication)
pFGFR1, 3 phosphorylation
BaF3-TEL-FGFR1
BaF3-TEL-FGFR3
DMPK
Tier 1 ADMET
Solubility
PPB
Permeability
h/r/m LM stability
hERG
Tier 2 ADMET
CYP450 Inhibition
CYP induction
h/r/m Hepatocyte stability
Caco-2 permeability
PK
PPB (fraction unbound)
CL
t1/2
Cmax
F%
Selectivity and MOA Study
pFGFR3 functional whole blood HTRF assay
pFGFR2 in KATO-III spiked whole blood ELISA assay
Inhibition of FGFR pathway
FRS2, Fibrolast growth factor receptor substrate 2
ERK, extracellular signal regulated kinase
pFRS2 and pERK
KMS-11(FGFR3 Y373C)
pFGFR and pERK
SNU-16 (FGFR2 amplification)
Panel
Cell proliferation
SW780 (FGFR3-BAIAP2L1)
OPM-2 (FGFR3 K650E)
KATO-III (FGFR2 amplification)
AN3CA (FGFR2 N310R/N549K)
BaF3-FGFR2-BICC1
BaF3-TEL-FGFR3 V555M
BaF3-TEL-FGFR3 V555L
In vivo Pharmacology
CDX model
Female NSG mice
PD
pFGFR3
pERK
pFRS2
Safety and IND study
Safety panel
Kinase panel
Cell panel
IND package
In vitro Pharmacology
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