Dabrafenib

ダブラフェニブ (Dabrafenib (GSK2118436、GSK2118436A)) は変異型 BRAF^V600E 特異的阻害剤 (無細胞アッセイで IC50 = 0.7 nM) であり、B-Raf(wt), c-Raf(wt) に対する効力は変異型に比べそれぞれ 7/9 倍低くなっています。

CAS No. 1195765-45-7

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
20mg	JPY 41500	国内在庫あり
50mg	JPY 71500	国内在庫あり
100mg	JPY 116500	国内在庫あり
1g	JPY 295500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（276）

製品安全説明書

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Dabrafenib関連製品

関連ターゲット	C-Raf/Raf-1 B-Raf A-raf	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library MAPK Inhibitor Library Cell Cycle compound library TGF-beta/Smad compound library Anti-alzheimer Disease Compound Library	もっと見る

シグナル伝達経路

Rafシグナル伝達経路

Raf阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
HuNS-1	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
IGROV1	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
HT-3	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
HT	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
HPAF-II	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
Hs746.T	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
HOS	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
HN5	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
HMCB	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
Hep3B	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
Hela	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
HCC-1954	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
HCC-70	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
G401	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
FaDu	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
EKVX	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
EFM-19	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
EB-3	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
DU-145	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
DOTC 24510	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
Daudi	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
CRO-AP2	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
COR-L23	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
Colo704	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
Colo320DM	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
CHL-1	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
CGTHW1	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
CaOV3	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
Calu-3	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
CAL-62	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
CAL-27	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
C33A	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
C-4 I	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
BxPc3	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
BT-20	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
Be(2)C	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
ARH-77	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
A2780	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
A431	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
A427	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
A204	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
A172	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
786-O	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
647-V	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
22Rv1	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
MES-SA	Growth Inhibition Assay	10 μM	72 h	IC50=6.989 μM	23844038
C3A	Growth Inhibition Assay	10 μM	72 h	IC50=5.414 μM	23844038
HL-60	Growth Inhibition Assay	10 μM	72 h	IC50=2.178 μM	23844038
HT-1080	Growth Inhibition Assay	10 μM	72 h	IC50=2.004 μM	23844038
GDM-1	Growth Inhibition Assay	10 μM	72 h	IC50=1.997 μM	23844038
CEM/C1	Growth Inhibition Assay	10 μM	72 h	IC50=1.773 μM	23844038
SNU-1	Growth Inhibition Assay	10 μM	72 h	IC50=1.501 μM	23844038
MC/CAR	Growth Inhibition Assay	10 μM	72 h	IC50=1.002 μM	23844038
RPMI-6666	Growth Inhibition Assay	10 μM	72 h	IC50=928 nM	23844038
DB	Growth Inhibition Assay	10 μM	72 h	IC50=873 nM	23844038
BC-1	Growth Inhibition Assay	10 μM	72 h	IC50=704 nM	23844038
H4	Growth Inhibition Assay	10 μM	72 h	IC50=619 nM	23844038
CESS	Growth Inhibition Assay	10 μM	72 h	IC50=497 nM	23844038
SK-MES-1	Growth Inhibition Assay	10 μM	72 h	IC50=329 nM	23844038
JRT3-T35	Growth Inhibition Assay	10 μM	72 h	IC50=295 nM	23844038
ACHN	Growth Inhibition Assay	10 μM	72 h	IC50=294 nM	23844038
BC-3	Growth Inhibition Assay	10 μM	72 h	IC50=277 nM	23844038
RPMI-8226	Growth Inhibition Assay	10 μM	72 h	IC50=263 nM	23844038
HuT78	Growth Inhibition Assay	10 μM	72 h	IC50=52 nM	23844038
BFTC-905	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SK-N-AS	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
CHP-212	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
LS1034	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
HCC-2998	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
Calu-6	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H460	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
T-84	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H747	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
HCT-116	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
DLD-1	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SW480	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SHP-77	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
A549	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
LS-174T	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
UMUC-3	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SW-837	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SW756	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
MDA-MB-231	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H508	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
OV-90	Growth Inhibition Assay	10 μM	72 h	IC50=29 nM	23844038
YUMAC	Growth Inhibition Assay	10 μM	72 h	IC50=5 nM	23844038
WM-115	Growth Inhibition Assay	10 μM	72 h	IC50=5 nM	23844038
GCT	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
A673	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
RKO	Growth Inhibition Assay	10 μM	72 h	IC50=2.522 μM	23844038
SW872	Growth Inhibition Assay	10 μM	72 h	IC50=377 nM	23844038
SW1417	Growth Inhibition Assay	10 μM	72 h	IC50=158 nM	23844038
HT-29	Growth Inhibition Assay	10 μM	72 h	IC50=66 nM	23844038
ES-2	Growth Inhibition Assay	10 μM	72 h	IC50=53 nM	23844038
A101D	Growth Inhibition Assay	10 μM	72 h	IC50=9 nM	23844038
SH-4	Growth Inhibition Assay	10 μM	72 h	IC50=8 nM	23844038
SK-MEL-3	Growth Inhibition Assay	10 μM	72 h	IC50=7 nM	23844038
Colo 205	Growth Inhibition Assay	10 μM	72 h	IC50=7 nM	23844038
UACC-257	Growth Inhibition Assay	10 μM	72 h	IC50=6 nM	23844038
DU-4475	Growth Inhibition Assay	10 μM	72 h	IC50=5 nM	23844038
A375	Growth Inhibition Assay	10 μM	72 h	IC50=4 nM	23844038
SK-MEL-28	Growth Inhibition Assay	10 μM	72 h	IC50=3 nM	23844038
M14	Growth Inhibition Assay	10 μM	72 h	IC50=2 nM	23844038
SK-MEL-1	Growth Inhibition Assay	10 μM	72 h	IC50=2 nM	23844038
C32TG	Growth Inhibition Assay	10 μM	72 h	IC50=1 nM	23844038
UACC-62	Growth Inhibition Assay	10 μM	72 h	IC50=1 nM	23844038
MALME-3M	Growth Inhibition Assay	10 μM	72 h	IC50=1 nM	23844038
A375P-F11	Growth Inhibition Assay	10 μM	72 h	Inhibition of B-Raf V600E mutant-driven A375P-F11 cell proliferation with IC50 of 0.071 μM	23844038
SK-MEL-28	Growth Inhibition Assay	10 μM	72 h	Inhibition of B-Raf V600E mutant-driven SK-MEL-28 cell proliferation with IC50 of 0.043 μM	23844038
HFF	Growth Inhibition Assay	10 μM	72 h	Inhibition of proliferation of human HFF cells harboring wild type B-Raf with IC50 of 3 μM	24900673
J82	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
JM1	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
Kato III	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
KHOS-240S	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
KM-12	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
KPL-1	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
KYSE-30	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
LNCaP	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
MCF-7	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
MC-IXC	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
MDA-MB-175 VII	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
MDA-MB-468	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
MiaPaCa	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
Molt-4	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-ADR/RES	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H69	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H82	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-N87	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H146	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H157	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H187	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H209	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H226	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H292	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H322	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H358	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H520	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H526	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H630	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H661	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H716	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H1563	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H1792	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H2030	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H2052	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H2122	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
NCI-H2228	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
OE-19	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
OE-21	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
OE-33	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
OVCAR-3	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
OVCAR-4	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
OVCAR-5	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
P3HR-1	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
PC-3	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
Raji	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
RD	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
RD-ES	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
RL	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SaOS2	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SCC-9	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SCC-12	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SCC-13	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SCC-15	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SCC-25	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SCLC-3	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SF-268	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SF-295	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SJRH30	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SK-BR-3	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SK-LMS-1	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SK-N-DZ	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SK-N-F1	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SKOV-3	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SK-UT-1	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SN12C	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SNB-19	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SNU-5	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SNU-16	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SNU-398	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SNU-449	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SR	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
ST486	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SW579	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SW684	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SW-780	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SW900	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SW1088	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SW1463	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
SW1990	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
T47D	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
TE381.T	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
TK-10	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
U2OS	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
U251	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
UACC-812	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
YAPC	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
ZR-75-1	Growth Inhibition Assay	10 μM	72 h	IC50=10 μM	23844038
A375	Function assay	1.2 μM	4 h	Inhibition of phosphorylation of MEK, ERK, and S6P	22389471
Colo-205	Function assay	1 μM	4 d	Induced a highly comparable compaction phenotype	25381152
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
RBW-1	Function assay	1 μM		No reduction of Mek 1/2 phosphorylation	24885690
RBO-1	Function assay	1 μM		Inhibition of Mek 1/2 phosphorylation	24885690
RBO-2	Function assay	1 μM		Inhibition of Mek 1/2 phosphorylation	24885690
RBOW	Function assay	1 μM		Inhibition of Mek 1/2 phosphorylation	24885690
HepG2	Function Assay		45 min	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
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
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
A375	Function assay		1 h	IC50 = 0.001 μM	27085672
MIAPaCa2	Function assay		1 h	EC50 = 0.529 μM	27085672
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
COLO205	Growth Inhibition Assay			Inhibition of human COLO205 cell proliferation with IC50 of 0.007 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
	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
YUSIT1	Function assay			reduced sensitivity with IC50 > 0.5 μM	22389471
MeWo	Growth inhibition assay			IC50 = 987 nM	26018524
WiDr	Growth inhibition assay			IC50 = 76 nM	26018524
HCT116	Function assay			IC50 = 5.88 μM	25965804
A375	Function assay			IC50 = 0.004 μM	29461827
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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生物活性

製品説明

ダブラフェニブ (Dabrafenib (GSK2118436、GSK2118436A)) は変異型 BRAF^V600E 特異的阻害剤 (無細胞アッセイで IC50 = 0.7 nM) であり、B-Raf(wt), c-Raf(wt) に対する効力は変異型に比べそれぞれ 7/9 倍低くなっています。

Targets

B-Raf (V600E) ^[3] (Cell-free assay)	B-Raf ^[3] (Cell-free assay)	C-Raf ^[3] (Cell-free assay)
0.7 nM	5.2 nM	6.3 nM

In Vitro
In vitro	Dabrafenib is selective for Raf kinase, with 400 fold selectivity towards B-Raf over 91% of the other kinases tested. Dabrafenib inhibits B-Raf^V600E kinase, leading to decreased ERK phosphorylation and inhibition of cell proliferationby an initial arrest in the G1 phase of the cell cycle in cancer cells that specifically encode the mutation for B-Raf^V600E. ^[1]
細胞実験	細胞株	A375PF11 cells
	濃度	> 10 uM
	反応時間	24 h
	実験の流れ	Cells were treated with different concentrations of drug for 24 h.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	β-catenin p-S6 / p-AKT308 / p-AKT473 pMEK / pERK / ERK		29167314
	Growth inhibition assay	IC50		24735930

In Vivo
In Vivo	Dabrafenib (orally administrated) inhibits the growth of B-RafV600E mutant melanoma (A375P) and colon cancer (Colo205) human tumor xenografts, growing subcutaneously in immuno-compromised mice. ^[1]
動物実験	動物モデル	Male C57Bl/6J mice
	投与量	3 mg/kg
	投与経路	Osmotic pumps

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT06079333	Recruiting	Anaplastic Thyroid Cancer	Leiden University Medical Center\|Novartis	January 1 2023	Phase 2
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	--

参考
[1] Sylvie Laquerre, et al. 2009, EORTC International Conference. Abst B88. [2] Greger JG, et al. Mol Cancer Ther, 2012, 11(4), 909-920. [3] Rheault TR, et al. ACS Med Chem Lett. 2013 Feb 7;4(3):358-62. [4] Meijles DN, et al. Clin Sci (Lond). 2021 Jul 30;135(14):1631-1647. + 展開

参考

[4] Meijles DN, et al. Clin Sci (Lond). 2021 Jul 30;135(14):1631-1647.

+ 展開

化学情報

分子量	519.56	化学式	C₂₃H₂₀F₃N₅O₂S₂
CAS No.	1195765-45-7	SDF	Download Dabrafenib SDFをダウンロードする
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
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (192.47 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.					投与溶液組成計算機
	Clear solution	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O	5.0mg/ml	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.	投与溶液組成計算機
Clear solution	2% DMSO 1 45% PEG300 2 2%Tween80 3 50%ddH2O	3.0mg/ml	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.
Clear solution	2%DMSO 1 Corn oil	3.0mg/ml	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.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):