Home MAPK Raf Inhibitor Dabrafenib (GSK2118436)

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Dabrafenib (GSK2118436) BRAF-Inhibitor

Kat.-Nr.S2807

Dabrafenib ist ein spezifischer Inhibitor der mutierten BRAFV600E mit einer IC50 von 0,7 nM in zellfreien Assays, mit 7- und 9-fach geringerer Wirksamkeit gegen B-Raf(wt) bzw. c-Raf.
Dabrafenib (GSK2118436) Raf Inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 519.56

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Qualitätskontrolle (Quality Control)

Charge: Reinheit: 99.99%
99.99

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung PMID
Kinase Assay Inhibition of N-terminal His tagged B-Raf V600E mutant expressed in baculovirus infected insect cells co-expressing CDC37 assessed as decrease in biotinylated-MEK protein phosphorylation by AlphaScreen assay with IC50 of 0.0007 μM 24900673
SK-MEL-28 Kinase Assay 1 h Inhibition of B-Raf V600E mutant in human SK-MEL-28 cells assessed as decrease in ERK phosphorylation with IC50 of 0.004 μM 24900673
HepG2 Kinase Assay Inhibition of B-Raf V600E mutant in human HepG2 cells assessed as decrease in ERK phosphorylation with IC50 of 0.004 μM 24900673
COLO205 Growth Inhibition Assay Inhibition of human COLO205 cell proliferation with IC50 of 0.007 μM 24900673
HepG2 Function Assay 45 min DMSO Inhibition of Alk5 in TGF-beta-stimulated human HepG2 cells assessed as decrease in Smad2 phosphorylation treated for 45 mins prior to TGF-beta stimulation measured after 60 mins by odyssey blot scanner analysis with IC50 of 3.7 μM 24900673
HFF Growth Inhibition Assay 10 μM 72 h DMSO Inhibition of proliferation of human HFF cells harboring wild type B-Raf with IC50 of 3 μM 24900673
SK-MEL-28 Growth Inhibition Assay 10 μM 72 h DMSO Inhibition of B-Raf V600E mutant-driven SK-MEL-28 cell proliferation with IC50 of 0.043 μM 23844038
A375P-F11 Growth Inhibition Assay 10 μM 72 h DMSO Inhibition of B-Raf V600E mutant-driven A375P-F11 cell proliferation with IC50 of 0.071 μM 23844038
MALME-3M Growth Inhibition Assay 10 μM 72 h DMSO IC50=1 nM 23844038
UACC-62 Growth Inhibition Assay 10 μM 72 h DMSO IC50=1 nM 23844038
C32TG Growth Inhibition Assay 10 μM 72 h DMSO IC50=1 nM 23844038
SK-MEL-1 Growth Inhibition Assay 10 μM 72 h DMSO IC50=2 nM 23844038
M14 Growth Inhibition Assay 10 μM 72 h DMSO IC50=2 nM 23844038
SK-MEL-28 Growth Inhibition Assay 10 μM 72 h DMSO IC50=3 nM 23844038
A375 Growth Inhibition Assay 10 μM 72 h DMSO IC50=4 nM 23844038
DU-4475 Growth Inhibition Assay 10 μM 72 h DMSO IC50=5 nM 23844038
UACC-257 Growth Inhibition Assay 10 μM 72 h DMSO IC50=6 nM 23844038
Colo 205 Growth Inhibition Assay 10 μM 72 h DMSO IC50=7 nM 23844038
SK-MEL-3 Growth Inhibition Assay 10 μM 72 h DMSO IC50=7 nM 23844038
SH-4 Growth Inhibition Assay 10 μM 72 h DMSO IC50=8 nM 23844038
A101D Growth Inhibition Assay 10 μM 72 h DMSO IC50=9 nM 23844038
ES-2 Growth Inhibition Assay 10 μM 72 h DMSO IC50=53 nM 23844038
HT-29 Growth Inhibition Assay 10 μM 72 h DMSO IC50=66 nM 23844038
SW1417 Growth Inhibition Assay 10 μM 72 h DMSO IC50=158 nM 23844038
SW872 Growth Inhibition Assay 10 μM 72 h DMSO IC50=377 nM 23844038
RKO Growth Inhibition Assay 10 μM 72 h DMSO IC50=2.522 μM 23844038
A673 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
GCT Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
WM-115 Growth Inhibition Assay 10 μM 72 h DMSO IC50=5 nM 23844038
YUMAC Growth Inhibition Assay 10 μM 72 h DMSO IC50=5 nM 23844038
OV-90 Growth Inhibition Assay 10 μM 72 h DMSO IC50=29 nM 23844038
NCI-H508 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
MDA-MB-231 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SW756 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SW-837 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
UMUC-3 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
LS-174T Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
A549 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SHP-77 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SW480 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
DLD-1 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
HCT-116 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H747 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
T-84 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H460 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
Calu-6 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
HCC-2998 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
LS1034 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
CHP-212 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SK-N-AS Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
BFTC-905 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
HuT78 Growth Inhibition Assay 10 μM 72 h DMSO IC50=52 nM 23844038
RPMI-8226 Growth Inhibition Assay 10 μM 72 h DMSO IC50=263 nM 23844038
BC-3 Growth Inhibition Assay 10 μM 72 h DMSO IC50=277 nM 23844038
ACHN Growth Inhibition Assay 10 μM 72 h DMSO IC50=294 nM 23844038
JRT3-T35 Growth Inhibition Assay 10 μM 72 h DMSO IC50=295 nM 23844038
SK-MES-1 Growth Inhibition Assay 10 μM 72 h DMSO IC50=329 nM 23844038
CESS Growth Inhibition Assay 10 μM 72 h DMSO IC50=497 nM 23844038
H4 Growth Inhibition Assay 10 μM 72 h DMSO IC50=619 nM 23844038
BC-1 Growth Inhibition Assay 10 μM 72 h DMSO IC50=704 nM 23844038
DB Growth Inhibition Assay 10 μM 72 h DMSO IC50=873 nM 23844038
RPMI-6666 Growth Inhibition Assay 10 μM 72 h DMSO IC50=928 nM 23844038
MC/CAR Growth Inhibition Assay 10 μM 72 h DMSO IC50=1.002 μM 23844038
SNU-1 Growth Inhibition Assay 10 μM 72 h DMSO IC50=1.501 μM 23844038
CEM/C1 Growth Inhibition Assay 10 μM 72 h DMSO IC50=1.773 μM 23844038
GDM-1 Growth Inhibition Assay 10 μM 72 h DMSO IC50=1.997 μM 23844038
HT-1080 Growth Inhibition Assay 10 μM 72 h DMSO IC50=2.004 μM 23844038
HL-60 Growth Inhibition Assay 10 μM 72 h DMSO IC50=2.178 μM 23844038
C3A Growth Inhibition Assay 10 μM 72 h DMSO IC50=5.414 μM 23844038
MES-SA Growth Inhibition Assay 10 μM 72 h DMSO IC50=6.989 μM 23844038
22Rv1 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
647-V Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
786-O Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
A172 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
A204 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
A427 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
A431 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
A2780 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
ARH-77 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
Be(2)C Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
BT-20 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
BxPc3 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
C-4 I Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
C33A Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
CAL-27 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
CAL-62 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
Calu-3 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
CaOV3 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
CGTHW1 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
CHL-1 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
Colo320DM Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
Colo704 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
COR-L23 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
CRO-AP2 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
Daudi Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
DOTC 24510 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
DU-145 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
EB-3 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
EFM-19 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
EKVX Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
FaDu Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
G401 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
HCC-70 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
HCC-1954 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
Hela Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
Hep3B Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
HMCB Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
HN5 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
HOS Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
HPAF-II Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
Hs746.T Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
HT Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
HT-3 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
HuNS-1 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
IGROV1 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
J82 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
JM1 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
Kato III Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
KHOS-240S Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
KM-12 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
KPL-1 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
KYSE-30 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
LNCaP Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
MCF-7 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
MC-IXC Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
MDA-MB-175 VII Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
MDA-MB-468 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
MiaPaCa Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
Molt-4 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-ADR/RES Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H69 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H82 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-N87 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H146 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H157 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H187 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H209 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H226 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H292 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H322 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H358 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H520 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H526 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H630 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H661 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H716 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H1563 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H1792 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H2030 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H2052 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H2122 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
NCI-H2228 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
OE-19 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
OE-21 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
OE-33 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
OVCAR-3 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
OVCAR-4 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
OVCAR-5 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
P3HR-1 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
PC-3 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
Raji Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
RD Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
RD-ES Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
RL Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SaOS2 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SCC-9 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SCC-12 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SCC-13 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SCC-15 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SCC-25 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SCLC-3 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SF-268 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SF-295 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SJRH30 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SK-BR-3 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SK-LMS-1 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SK-N-DZ Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SK-N-F1 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SKOV-3 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SK-UT-1 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SN12C Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SNB-19 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SNU-5 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SNU-16 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SNU-398 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SNU-449 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SR Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
ST486 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SW579 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SW684 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SW-780 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SW900 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SW1088 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SW1463 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
SW1990 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
T47D Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
TE381.T Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
TK-10 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
U2OS Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
U251 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
UACC-812 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
YAPC Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
ZR-75-1 Growth Inhibition Assay 10 μM 72 h DMSO IC50=10 μM 23844038
A375 Function assay 1.2 μM 4 h DMSO Inhibition of phosphorylation of MEK, ERK, and S6P 22389471
YUSIT1 Function assay DMSO reduced sensitivity with IC50 > 0.5 μM 22389471
MeWo Growth inhibition assay DMSO IC50 = 987 nM 26018524
WiDr Growth inhibition assay DMSO IC50 = 76 nM 26018524
Colo-205 Function assay 1 μM 4 d DMSO Induced a highly comparable compaction phenotype 25381152
RBW-1 Function assay 1 μM DMSO No reduction of Mek 1/2 phosphorylation 24885690
RBO-1 Function assay 1 μM DMSO Inhibition of Mek 1/2 phosphorylation 24885690
RBO-2 Function assay 1 μM DMSO Inhibition of Mek 1/2 phosphorylation 24885690
RBOW Function assay 1 μM DMSO Inhibition of Mek 1/2 phosphorylation 24885690
M257 Growth Inhibition Assay 100 nM 72 h Does not inhibit proliferation of M257 cell harbouring wild type BRAF 23317446
LCP Growth Inhibition Assay 100 nM 72 h Inhibition of proliferation of LCP cell harbouring BRAF V600R mutantation 23317446
WM266 Growth Inhibition Assay 100 nM 72 h Inhibition of proliferation of WM266 cell harbouring BRAF V601D mutantation 23317446
M257 Growth Inhibition Assay 100 nM 72 h Does not inhibit ERK1-2 phosphorylation in M257 cell harbouring wild type BRAF 23317446
LCP Growth Inhibition Assay 100 nM 72 h Inhibit ERK1-2 phosphorylation in LCP cell harbouring BRAF V600R mutantation 23317446
WM266 Growth Inhibition Assay 100 nM 72 h Inhibit ERK1-2 phosphorylation in WM266 cell harbouring BRAF V600D mutantation 23317446
A375 BRAF competitive binding assay 15 min IC50 = 0.006 μM 25965804
A375 Function assay 72 h IC50 = 0.011 μM 25965804
A375 ARAF competitive binding assay 15 min IC50 = 0.026 μM 25965804
A375 CRAF competitive binding assay 15 min IC50 = 0.15 μM 25965804
HCT116 Function assay IC50 = 5.88 μM 25965804
A375 Function assay 1 h IC50 = 0.001 μM 27085672
MIAPaCa2 Function assay 1 h EC50 = 0.529 μM 27085672
A375 Function assay IC50 = 0.004 μM 29461827
SK-MEL-28 Cytotoxicity assay 72 h IC50 = 0.043 μM 29461827
Sf9 Function assay 60 min IC50 = 0.009 μM 27774137
SK-MEL-28 Growth inhibition assay 48 h Growth inhibition of human SK-MEL-28 cells harboring BRAF V600E mutant measured after 48 hrs resazurin assay 27774137
SK-MEL-28 Growth inhibition assay 48 h Growth inhibition of human SK-MEL-28 cells harboring BRAF V600E mutant preincubated for 1 hr followed by irradiation of 1.13 kW/m2 UV-light for 5 mins measured after 48 hrs resazurin assay 27774137
SK-MEL-28 Cytotoxicity assay 48 h Cytostatic activity in human SK-MEL-28 cells harboring BRAF V600E mutant at 1 and 30 uM measured after 48 hrs resazurin assay 27774137
DAOY Primary screen assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
NB1643 Primary screen assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
SK-N-MC Primary screen assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
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Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Molekulargewicht 519.56 Formel

C23H20F3N5O2S2

 Lagerung (Ab dem Eingangsdatum)
CAS-Nr. 1195765-45-7 SDF herunterladen Lagerung von Stammlösungen

Synonyme GSK2118436, GSK2118436A Smiles CC(C)(C)C1=NC(=C(S1)C2=NC(=NC=C2)N)C3=C(C(=CC=C3)NS(=O)(=O)C4=C(C=CC=C4F)F)F

Löslichkeit (Solubility)

In vitro
Charge:

DMSO : 100 mg/mL (192.47 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewichtsrechner

In vivo
Charge:

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

mg/kg g μL

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.

Wirkmechanismus (Mechanism of Action)

Targets/IC50/Ki
B-Raf (V600E)
(Cell-free assay)
0.7 nM
B-Raf
(Cell-free assay)
5.2 nM
C-Raf
(Cell-free assay)
6.3 nM
In vitro

Dabrafenib ist selektiv für Raf-Kinase, mit einer 400-fachen Selektivität gegenüber B-Raf im Vergleich zu 91% der anderen getesteten Kinasen. Diese Verbindung hemmt die B-RafV600E-Kinase, was zu einer verminderten ERK-Phosphorylierung und Hemmung der Zellproliferation durch einen anfänglichen Arrest in der G1-Phase des Zellzyklus in Krebszellen führt, die spezifisch die Mutation für B-RafV600E kodieren.

In vivo

Dabrafenib (oral verabreicht) hemmt das Wachstum von B-RafV600E-mutiertem Melanom (A375P) und Darmkrebs (Colo205) menschlichen Tumor-Xenografts, die subkutan in immungeschwächten Mäusen wachsen.

Literatur
  • [4] https://pubmed.ncbi.nlm.nih.gov/34296750/

Anwendungen (Applications)

Methoden Biomarker Bilder PMID
Western blot pMEK / pERK / ERK p-S6 / p-AKT308 / p-AKT473 β-catenin
S2807-WB1
31158244
Growth inhibition assay IC50
S2807-IC50
24735930

Klinische Studieninformationen (Clinical Trial Information)

(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)

NCT-Nummer Rekrutierung Erkrankungen Sponsor/Kooperationspartner Startdatum Phasen
NCT06079333 Recruiting
Anaplastic Thyroid Cancer
Leiden University Medical Center|Novartis
 January 1 2023 Phase 2
NCT06337617 Completed
BRAF V600 Mutation Positive Melanoma
Novartis Pharmaceuticals|Novartis
 May 10 2022 --
NCT04961619 Recruiting
Melanoma
Novartis Pharmaceuticals|Novartis
 December 1 2021 --
NCT04547946 Completed
Malignant Melanoma
Novartis Pharmaceuticals|Novartis
 October 15 2021 --
NCT05171374 Recruiting
Melanoma Stage III|Melanoma Stage IV|Melanoma
MelanomaPRO Russia|Novartis
 September 30 2021 --