Dabrafenib | GSK2118436A;GSK2118436 | 达拉菲尼 | Raf

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达拉非尼 /Dabrafenib {[allProObj[0].p_purity_real_show]}

货号：A484347 同义名： 达拉菲尼 / GSK2118436A;GSK2118436

Dabrafenib (GSK2118436A) 是一种 ATP 竞争性的 Raf 抑制剂，对 C-Raf 和 B-RafV600E 的 IC50 值分别为 5 nM 和 0.6 nM。

Dabrafenib 化学结构
CAS号：1195765-45-7

Dabrafenib 3D分子结构
CAS号：1195765-45-7

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Dabrafenib 纯度/质量文件产品仅供科研

货号：A484347 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

Raf 亚型比较

产品名称	A-raf ↓ ↑	B-Raf ↓ ↑	C-Raf/Raf-1 ↓ ↑	Raf ↓ ↑	其他靶点	纯度
Encorafenib		✔				99%+
GDC-0879		++++ B-Raf, IC50: 0.13 nM				99%+
SB-590885		++++ B-Raf, Ki: 0.16 nM				99%+
RAF265						99%+
Dabrafenib		++++ B-Raf, IC50: 5.2 nM B-Raf (V600E), IC50: 0.7 nM	+++ C-Raf, IC50: 6.3 nM			98%
Lifirafenib	++++ WT A-RAF, IC50: 1 nM	++ BRAF(V600E), IC50: 23 nM BRAF WT, IC50: 32 nM	+++ C-RAF (Y340/341D), IC50: 7 nM		EGFR	98%
ZM 336372			+ C-Raf, IC50: 70 nM			99%+
NVP-BHG 712			+ C-Raf, IC50: 0.395 μM			99%+
CCT196969		+ BRAF, IC50: 0.1 μM	++ CRAF, IC50: 0.01 μM		Src	98%
Vemurafenib		++ B-Raf, IC50: 100 nM B-Raf (V600E), IC50: 31 nM	+ C-Raf, IC50: 48 nM			98+%
PLX4720		++ B-Raf, IC50: 160 nM B-Raf (V600E), IC50: 13 nM	+++ C-Raf-1 (Y340D/Y341D), IC50: 6.7 nM		BRK	99+%
GW 5074			+++ C-Raf, IC50: 9 nM			99%+
Avutometinib		+++ BRAF V600E, IC50: 8.2 nM BRAF, IC50: 19 nM	+ CRAF, IC50: 56 nM			98%
LY3009120		++++ BRAF(V600E), IC50: 5.8 nM BRAF WT, IC50: 15 nM	++++ C-Raf, IC50: 4.3 nM			99%+
Agerafenib		++ B-Raf (V600E), Kd: 14 nM B-Raf, Kd: 36 nM	+ C-Raf, Kd: 39 nM		RET	99%+
TAK-632		+++ B-Raf, IC50: 8.3 nM	++++ C-Raf, IC50: 1.4 nM			99%+
AZ 628		+ B-Raf, IC50: 105 nM B-Raf (V600E), IC50: 34 nM	++ C-Raf-1, IC50: 29 nM			99%
PLX7904				✔		98+%
Sorafenib		++ B-Raf (V599E), IC50: 38 nM B-Raf, IC50: 22 nM	++++ Raf-1, IC50: 6 nM	++++ Raf-1, IC50: 6 nM		99%
Tovorafenib				✔		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Dabrafenib 生物活性

靶点	B-Raf B-Raf, IC50:5.2 nM B-Raf (V600E), IC50:0.7 nM C-Raf/Raf-1 C-Raf, IC50:6.3 nM
描述	The RAS/RAF signaling pathway is an important mediator of tumor cell proliferation and angiogenesis. Among them, B-RAF is the most frequently mutated protein kinase in human cancers. Dabrafenib is a potent, selective and efficacious inhibitor of B-Raf^V600E with IC₅₀ value of 0.7 nM, and less potent to B-Raf and C-Raf with IC₅₀ values of 5.2 nM and 6.3 nM (measured by enzymatic activity), respectively. Consistent with the in vitro kinase assay, Dabrafenib displayed compelling inhibitory on p-ERK in SKMEL28 cells with IC₅₀ value of 4 nM, as well as on cell proliferation of B-Raf^V600E-driven melanoma lines such as SKMEL28 and A375P F11 (IC₅₀=3 nM and 8 nM, respectively) and colorectal carcinoma line Colo205 (IC₅₀=7 nM). Meanwhile, Dabrafenib had a minimal effect on cells with wild-type B-Raf (HFF IC₅₀=3.0 μM) and in tumor cells not harboring the activating B-Raf^V600E mutation. Oral administration of Dabrafenib at doses of 0.1, 1, 10, and 100 mg/kg once daily for 14 days dose-dependently reduce tumor growth with notable pharmacodynamic response, measured by pERK levels after a single oral dose, in CD1 nu/nu mice bearing A375P F11 (B-Raf^V600E) tumors. Dabrafenib is currently in phase III clinical development for the treatment of activating B-Raf mutant tumors^[1].
作用机制	Dabrafenib binding to BRAF is ATP-competitive.^[2]

Dabrafenib 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
22Rv1	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
647-V	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
786-O	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
A101D	10 μM	Growth Inhibition Assay	72 h	IC50=9 nM	23844038

Dabrafenib 动物研究

Dose

Mice: 0.3 mg/kg - 100 mg/kg^[2] (p.o.) Dog: 1 mg/kg - 50 mg/kg^[3] (p.o.) Rat: 5 mg/kg - 200 mg/kg^[3] (p.o.)

Administration

p.o.

Pharmacokinetics

Animal	Rats^[3]
Dose	20 mg/kg
Administration	p.o.
C_max	9.4 - 11.8 µg/ml
T_max	0.5 - 1 h
AUC_0→t	19.2 - 24.3 µg·h/ml

Dabrafenib 参考文献

[1]Rheault TR, Stellwagen JC, et al. Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors. ACS Med Chem Lett. 2013 Feb 7;4(3):358-62.

[2]King AJ, Arnone MR, et al. Dabrafenib; preclinical characterization, increased efficacy when combined with trametinib, while BRAF/MEK tool combination reduced skin lesions. PLoS One. 2013 Jul 3;8(7):e67583.

[3]Tafinlar

Dabrafenib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.92mL

0.38mL

0.19mL

9.62mL

1.92mL

0.96mL

19.25mL

3.85mL

1.92mL

Dabrafenib 技术信息

CAS号	1195765-45-7
分子式	C₂₃H₂₀F₃N₅O₂S₂
分子量	519.562

别名	达拉菲尼 ;GSK2118436A;GSK2118436
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 35 mg/mL(67.36 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

2% DMSO+45% PEG 300+2% Tween 80+water 5 mg/mL

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

22Rv1	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
647-V	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
786-O	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
A101D	10 μM	Growth Inhibition Assay	72 h	IC50=9 nM	23844038
A172	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
A204	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
A2780	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
A375	10 μM	Growth Inhibition Assay	72 h	IC50=4 nM	23844038
A375	1.2 μM	Function assay	4 h	Inhibition of phosphorylation of MEK, ERK, and S6P	22389471
A375P-F11	10 μM	Growth Inhibition Assay	72 h	Inhibition of B-Raf V600E mutant-driven A375P-F11 cell proliferation with IC50 of 0.071 μM	23844038
A427	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
A431	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
A549	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
A673	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
ACHN	10 μM	Growth Inhibition Assay	72 h	IC50=294 nM	23844038
ARH-77	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
BC-1	10 μM	Growth Inhibition Assay	72 h	IC50=704 nM	23844038
BC-3	10 μM	Growth Inhibition Assay	72 h	IC50=277 nM	23844038
Be(2)C	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
BFTC-905	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
BT-20	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
BxPc3	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
C32TG	10 μM	Growth Inhibition Assay	72 h	IC50=1 nM	23844038
C33A	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
C3A	10 μM	Growth Inhibition Assay	72 h	IC50=5.414 μM	23844038
C-4 I	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
CAL-27	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
CAL-62	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
Calu-3	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
Calu-6	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
CaOV3	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
CEM/C1	10 μM	Growth Inhibition Assay	72 h	IC50=1.773 μM	23844038
CESS	10 μM	Growth Inhibition Assay	72 h	IC50=497 nM	23844038
CGTHW1	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
CHL-1	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
CHP-212	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
Colo 205	10 μM	Growth Inhibition Assay	72 h	IC50=7 nM	23844038
COLO205		Growth Inhibition Assay		Inhibition of human COLO205 cell proliferation with IC50 of 0.007 μM	24900673
Colo-205	1 μM	Function assay	4 d	Induced a highly comparable compaction phenotype	25381152
Colo320DM	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
Colo704	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
COR-L23	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
CRO-AP2	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
Daudi	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
DB	10 μM	Growth Inhibition Assay	72 h	IC50=873 nM	23844038
DLD-1	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
DOTC 24510	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
DU-145	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
DU-4475	10 μM	Growth Inhibition Assay	72 h	IC50=5 nM	23844038
EB-3	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
EFM-19	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
EKVX	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
ES-2	10 μM	Growth Inhibition Assay	72 h	IC50=53 nM	23844038
FaDu	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
G401	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
GCT	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
GDM-1	10 μM	Growth Inhibition Assay	72 h	IC50=1.997 μM	23844038
H4	10 μM	Growth Inhibition Assay	72 h	IC50=619 nM	23844038
HCC-1954	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
HCC-2998	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
HCC-70	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
HCT-116	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
Hela	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
Hep3B	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
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
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
HFF	10 μM	Growth Inhibition Assay	72 h	Inhibition of proliferation of human HFF cells harboring wild type B-Raf with IC50 of 3 μM	23844038
HL-60	10 μM	Growth Inhibition Assay	72 h	IC50=2.178 μM	23844038
HMCB	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
HN5	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
HOS	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
HPAF-II	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
Hs746.T	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
HT	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
HT-1080	10 μM	Growth Inhibition Assay	72 h	IC50=2.004 μM	23844038
HT-29	10 μM	Growth Inhibition Assay	72 h	IC50=66 nM	23844038
HT-3	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
HuNS-1	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
HuT78	10 μM	Growth Inhibition Assay	72 h	IC50=52 nM	23844038
IGROV1	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
J82	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
JM1	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
JRT3-T35	10 μM	Growth Inhibition Assay	72 h	IC50=295 nM	23844038
Kato III	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
KHOS-240S	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
KM-12	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
KPL-1	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
KYSE-30	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
LCP	100 nM	Growth Inhibition Assay	72 h	Inhibition of proliferation of LCP cell harbouring BRAF V600R mutantation	23317446
LCP	100 nM	Growth Inhibition Assay	72 h	Inhibit ERK1-2 phosphorylation in LCP cell harbouring BRAF V600R mutantation	23317446
LNCaP	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
LS1034	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
LS-174T	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
M14	10 μM	Growth Inhibition Assay	72 h	IC50=2 nM	23844038
M257	100 nM	Growth Inhibition Assay	72 h	Does not inhibit proliferation of M257 cell harbouring wild type BRAF	23317446
M257	100 nM	Growth Inhibition Assay	72 h	Does not inhibit ERK1-2 phosphorylation in M257 cell harbouring wild type BRAF	23317446
MALME-3M	10 μM	Growth Inhibition Assay	72 h	IC50=1 nM	23844038
MC/CAR	10 μM	Growth Inhibition Assay	72 h	IC50=1.002 μM	23844038
MCF-7	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
MC-IXC	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
MDA-MB-175 VII	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
MDA-MB-231	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
MDA-MB-468	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
MES-SA	10 μM	Growth Inhibition Assay	72 h	IC50=6.989 μM	23844038
MeWo		Growth inhibition assay		IC50 = 987 nM	26018524
MiaPaCa	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
Molt-4	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-ADR/RES	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H146	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H1563	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H157	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H1792	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H187	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H2030	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H2052	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H209	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H2122	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H2228	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H226	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H292	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H322	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H358	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H460	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H508	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H520	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H526	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H630	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H661	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H69	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H716	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H747	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-H82	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
NCI-N87	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
OE-19	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
OE-21	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
OE-33	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
OV-90	10 μM	Growth Inhibition Assay	72 h	IC50=29 nM	23844038
OVCAR-3	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
OVCAR-4	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
OVCAR-5	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
P3HR-1	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
PC-3	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
Raji	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
RBO-1	1 μM	Function assay		Inhibition of Mek 1/2 phosphorylation	24885690
RBO-2	1 μM	Function assay		Inhibition of Mek 1/2 phosphorylation	24885690
RBOW	1 μM	Function assay		Inhibition of Mek 1/2 phosphorylation	24885690
RBW-1	1 μM	Function assay		No reduction of Mek 1/2 phosphorylation	24885690
RD	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
RD-ES	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
RKO	10 μM	Growth Inhibition Assay	72 h	IC50=2.522 μM	23844038
RL	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
RPMI-6666	10 μM	Growth Inhibition Assay	72 h	IC50=928 nM	23844038
RPMI-8226	10 μM	Growth Inhibition Assay	72 h	IC50=263 nM	23844038
SaOS2	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SCC-12	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SCC-13	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SCC-15	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SCC-25	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SCC-9	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SCLC-3	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SF-268	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SF-295	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SH-4	10 μM	Growth Inhibition Assay	72 h	IC50=8 nM	23844038
SHP-77	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SJRH30	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SK-BR-3	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SK-LMS-1	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SK-MEL-1	10 μM	Growth Inhibition Assay	72 h	IC50=2 nM	23844038
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
SK-MEL-28	10 μM	Growth Inhibition Assay	72 h	Inhibition of B-Raf V600E mutant-driven SK-MEL-28 cell proliferation with IC50 of 0.043 μM	23844038
SK-MEL-28	10 μM	Growth Inhibition Assay	72 h	IC50=3 nM	23844038
SK-MEL-3	10 μM	Growth Inhibition Assay	72 h	IC50=7 nM	23844038
SK-MES-1	10 μM	Growth Inhibition Assay	72 h	IC50=329 nM	23844038
SK-N-AS	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SK-N-DZ	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SK-N-F1	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SKOV-3	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SK-UT-1	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SN12C	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SNB-19	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SNU-1	10 μM	Growth Inhibition Assay	72 h	IC50=1.501 μM	23844038
SNU-16	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SNU-398	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SNU-449	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SNU-5	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SR	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
ST486	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SW1088	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SW1417	10 μM	Growth Inhibition Assay	72 h	IC50=158 nM	23844038
SW1463	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SW1990	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SW480	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SW579	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SW684	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SW756	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SW-780	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SW-837	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
SW872	10 μM	Growth Inhibition Assay	72 h	IC50=377 nM	23844038
SW900	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
T47D	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
T-84	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
TE381.T	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
TK-10	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
U251	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
U2OS	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
UACC-257	10 μM	Growth Inhibition Assay	72 h	IC50=6 nM	23844038
UACC-62	10 μM	Growth Inhibition Assay	72 h	IC50=1 nM	23844038
UACC-812	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
UMUC-3	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
WiDr		Growth inhibition assay		IC50 = 76 nM	26018524
WM-115	10 μM	Growth Inhibition Assay	72 h	IC50=5 nM	23844038
WM266	100 nM	Growth Inhibition Assay	72 h	Inhibition of proliferation of WM266 cell harbouring BRAF V601D mutantation	23317446
WM266	100 nM	Growth Inhibition Assay	72 h	Inhibit ERK1-2 phosphorylation in WM266 cell harbouring BRAF V600D mutantation	23317446
YAPC	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
YUMAC	10 μM	Growth Inhibition Assay	72 h	IC50=5 nM	23844038
YUSIT1		Function assay		reduced sensitivity with IC50 > 0.5 μM	22389471
ZR-75-1	10 μM	Growth Inhibition Assay	72 h	IC50=10 μM	23844038
		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

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B-Raf	B-Raf, IC50:5.2 nM B-Raf (V600E), IC50:0.7 nM
C-Raf/Raf-1	C-Raf, IC50:6.3 nM

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Dabrafenib 纯度/质量文件产品仅供科研