Dabrafenib

别名: GSK2118436, GSK2118436A 中文名称：达拉菲尼,达拉非尼

目录号：S2807 Purity: 99.99%

Dabrafenib是一种突变型BRAF^V600E特异性抑制剂，无细胞试验中IC50为0.7 nM，作用于B-Raf(wt)和c-Raf效果分别低7和9倍。

Dabrafenib Chemical Structure

CAS: 1195765-45-7

规格	价格	库存
10mM (1mL in DMSO)	892.71	现货
5mg	733.64	现货
20mg	1394.46	现货
50mg	2235.84	现货
100mg	3261.37	现货
1g	9582.3	现货
更大包装有超大折扣
400-668-6834 info@selleck.cn

产品质控

批次：纯度： 99.99%

99.99

Dabrafenib相关产品

相关靶点	C-Raf/Raf-1 B-Raf A-raf	点击展开
相关产品	PLX-4720 LY3009120 AZ 628 GDC-0879 SB590885 TAK-632 RAF265 (CHIR-265) GW5074 Avutometinib PLX7904 Plixorafenib (PLX8394) ZM 336372 Tovorafenib (MLN2480) Agerafenib (CEP-32496) Lifirafenib (BGB-283) Naporafenib (LXH254) Belvarafenib RAF709 B-Raf inhibitor 1 (Compound 13) dihydrochloride CCT196969	点击展开
相关化合物库	激酶抑制剂库 MAPK抑制剂库细胞周期化合物库 TGF-beta/Smad信号通路库抗阿尔茨海默病化合物库	点击展开

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息(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
点击查看更多细胞系数据

生物活性

产品描述

Dabrafenib是一种突变型BRAF^V600E特异性抑制剂，无细胞试验中IC50为0.7 nM，作用于B-Raf(wt)和c-Raf效果分别低7和9倍。

靶点

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

体外研究(In Vitro)
体外研究活性	Dabrafenib对Raf激酶具有选择性，对B-Raf的活性比其它测试过的91%的激酶高400倍。 Dabrafenib抑制B-Raf^V600E激酶，导致ERK磷酸化降低和抑制细胞的增值，在特异性编码突变的B-Raf^V600E的癌细胞中细胞停滞在G1期。
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	pMEK / pERK / ERK p-S6 / p-AKT308 / p-AKT473 β-catenin		31158244
	Growth inhibition assay	IC50		24735930

体内研究(In Vivo)
体内研究活性	Dabrafenib（口服）抑制B-RafV600E突变的黑色素瘤（A375P）的生长，在免疫受损小鼠中皮下注射结肠癌（Colo205），Dabrafenib（口服）同样能抑制肿瘤生长。 ^[1]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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	--

参考文献
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 https://pubmed.ncbi.nlm.nih.gov/22389471/ https://pubmed.ncbi.nlm.nih.gov/24900673/ https://pubmed.ncbi.nlm.nih.gov/34296750/ + 展开

参考文献

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
https://pubmed.ncbi.nlm.nih.gov/22389471/
https://pubmed.ncbi.nlm.nih.gov/24900673/

https://pubmed.ncbi.nlm.nih.gov/34296750/

+ 展开

化学信息&溶解度

分子量	519.56	分子式	C₂₃H₂₀F₃N₅O₂S₂
CAS号	1195765-45-7	SDF	Download Dabrafenib SDF
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
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 100 mg/mL ( (192.47 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL ( (192.47 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 91 mg/mL ( (175.14 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 4 mg/mL (7.69 mM)

Water : Insoluble

DMSO : 100 mg/mL ( (192.47 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL ( (192.47 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解配方批次：现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂				动物体内配方计算器
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	5.000mg/ml (9.62mM)	以 1 mL 工作液为例，取 50 μL 100 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀使其澄清；向上述体系中加入50 μL Tween-80，混合均匀使其澄清；然后继续加入 500 μLddH2O定容至 1 mL。工作液请现配现用！
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	2%DMSO 1 Corn oil 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	3.000mg/ml (5.77mM)	以 1 mL 工作液为例，取20μL150mg/ml的澄清DMSO储备液加到980μL玉米油中，混合均匀。工作液请现配现用！
澄清溶液	2% DMSO 1 45% PEG300 2 2%Tween80 3 50%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	3.000mg/ml (5.77mM)	以 1 mL 工作液为例，取20 μL 150 mg/ml的澄清DMSO储备液加到450 μL PEG300中，混合均匀使其澄清；向上述体系中加入20 μL Tween-80，混合均匀使其澄清；然后继续加入510 μL ddH2O定容至 1 mL。工作液请现配现用！
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	6.000mg/ml (11.55mM)	以 1 mL 工作液为例,取50μL120mg/ml的澄清DMSO储备液加到400μLPEG300中,混合均匀使其澄清;向上述体系中加入50μLTween80,混合均匀使其澄清;然后继续加入500μLddH2O定容至1mL。工作液请现配现用!

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

* 必填项

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):

Dabrafenib

产品质控

Dabrafenib相关产品

相关信号通路图

细胞实验数据示例

生物活性

化学信息&溶解度

实验计算

技术支持