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Dabrafenib (GSK2118436) BRAF-remmer

Name: Dabrafenib (GSK2118436)
Brand: Selleck Chemicals
SKU: S2807
Rating: 5 (319 reviews)

Cat.nr.S2807

Dabrafenib is een mutante BRAF^V600E-specifieke remmer met een IC50 van 0,7 nM in celvrije assays, met respectievelijk 7- en 9-voudig minder potentie tegen B-Raf(wt) en c-Raf.

Dabrafenib (GSK2118436) Raf remmer Chemical Structure

Chemische structuur

Molecuulgewicht: 519.56

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Batch: Zuiverheid: 99.99%

99.99

Gerelateerde doelwitten	ERK p38 MAPK JNK MEK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase
Overig Raf Inhibitoren	LY3009120 Exarafenib (KIN-2787) GDC-0879 Avutometinib (Ro5126766, CH5126766) PLX-4720 AZ 628 SB590885 TAK-632 GW5074 RAF265 (CHIR-265)

Celkweek, behandeling & werkzame concentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Formulering	Activiteitsbeschrijving	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
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit

Molecuulgewicht	519.56	Formule	C₂₃H₂₀F₃N₅O₂S₂	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	1195765-45-7	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	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

Oplosbaarheid

In vitro
Batch:

DMSO : 100 mg/mL (192.47 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	5.000mg/ml (9.62mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/mL clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify; add 50 μL of Tween-80 to the above system, mix evenly to clarify; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	3.000mg/ml (5.77mM)	Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clear DMSO stock solution to 980 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	2% DMSO 1 45% PEG300 2 2%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	3.000mg/ml (5.77mM)	Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clarified DMSO stock solution to 450 μL PEG300, mix evenly to clarify it; add 20 μL Tween-80 to the above system, mix evenly to clarify it; Then continue to add 510 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	6.000mg/ml (11.55mM)	Taking the 1 mL working solution as an example, add 50 μL of 120 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

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 is selectief voor Raf-kinase, met een 400-voudige selectiviteit voor B-Raf ten opzichte van 91% van de andere geteste kinasen. Deze verbinding remt B-Raf^V600E-kinase, wat leidt tot verminderde ERK-fosforylatie en remming van celproliferatie door een initiële arrest in de G1-fase van de celcyclus in kankercellen die specifiek de mutatie voor B-Raf^V600E coderen.
In vivo	Dabrafenib (oraal toegediend) remt de groei van B-RafV600E mutante melanoom (A375P) en darmkanker (Colo205) humane tumor xenografts, subcutaan groeiend in immuungecompromitteerde muizen.
Referenties	[1] https://www.researchgate.net/publication/269940032_Abstract_B88_A_selective_Raf_kinase_inhibitor_induces_cell_death_and_tumor_regression_of_human_cancer_cell_lines_encoding_B-RafV600E_mutation [2] https://pubmed.ncbi.nlm.nih.gov/22389471/ [3] https://pubmed.ncbi.nlm.nih.gov/24900673/ [4] https://pubmed.ncbi.nlm.nih.gov/34296750/

Toepassingen

Methoden	Biomarkers	Afbeeldingen	PMID
Western blot	pMEK / pERK / ERK p-S6 / p-AKT308 / p-AKT473 β-catenin		31158244
Growth inhibition assay	IC50		24735930

Informatie over klinische proeven

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
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	--

Technische ondersteuning

Gebruiksaanwijzing

Tel: +1-832-582-8158 Ext:3

Als u nog andere vragen heeft, laat dan een bericht achter.

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