Table 1.

In vitro cellular profile of sorafenib

Cellular assayMutational statusHistologic typeReference
Inhibition of pERK signaling
A375b-raf V600EMelanoma83
ATCb-raf V600EThyroid47
Bx PCWT-Ras, WT-B-RafPancreatic27
Colo829b-raf V600EMelanoma83
HepG2k-rasHCC35
LOXb-raf V600EMelanoma27
MDA-MB-231b-raf (G463V)/k-rasBreast27
PLC/PRF/5k-rasHCC46
U937UnknownLeukemia84
UACC 903b-raf V600EMelanoma74
WM-266-4b-raf V600DMelanoma83
Inhibition of tumor cell proliferation
ATCb-raf V600EThyroid47
EOL-1Flt-1 3 ITDLeukemia14
HepG2k-rasHCC27
HepG2k-rasHCC46
MDA-MB-231b-raf (G463V)/k-rasBreast27
MV4;11Flt-1 3 ITDLeukemia14
PLC/PRF/5k-rasHCC46
RS4-11Flt-1 WTLeukemia14
UACC 903b-raf V600EMelanoma75
SK-MEL 2n-rasMelanoma78
SK-MEL 28b-raf V600EMelanoma78
A2058b-raf V600EMelanoma78
Inhibition of receptor tyrosine kinase autophosphorylation
c-Kit T670IKit29, 30, 33
Flt-3 ITDFlt-314, 33
PDGF-β dependentPDGFR-β wt27
Mutant PDGFR-βETV6-PDGFRβ33
VEGF-dependentVEGFR-227
RETPTC3, C634R, M918T, V804L, V804M15, 31
Down-regulation of Mcl-1 in tumor cells
786-OVHL-/-RCC85
A549k-rasNSCLC38
ACHNUnknownRCC38
HT-29b-raf V600EColon38
JurkatUnknownLeukemia84
MDA-MB-231b-raf (G463V)/k-rasBreast38
U937UnknownLeukemia85
Induction of apoptosis in tumor cells
A549k-rasNSCLC38
EOL-1Flt-3 ITDLeukemia14
HepG2k-ras/unknownHCC46
KMCHUnknownCholangiocarcinoma38
MDA-MB-231b-raf (G463V)/k-rasBreast38
MV4;11Flt-3 ITDLeukemia14
PLC/PRF/5k-rasHCC46
U937UnknownLeukemia84