Ambeed 大中华区 CN | ZH

中文 - ZH English - EN

Ambeed.cn

搜索

关键字搜索批量搜索

首页 收藏 购物车0
首页 /
抑制剂/激动剂
细胞生物学 肿瘤
/
细胞培养
MAPK/ERK Pathway 肿瘤生长增殖和凋亡 乳腺癌 胃癌 肝癌 胰腺癌 结直肠癌
/
类器官培养添加剂
Raf
/ Dabrafenib/达拉非尼

Dabrafenib/达拉非尼 {[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/达拉非尼 化学结构 CAS号：1195765-45-7
Dabrafenib/达拉非尼 化学结构
CAS号：1195765-45-7
Dabrafenib/达拉非尼 3D分子结构
CAS号：1195765-45-7
Dabrafenib/达拉非尼 化学结构 CAS号：1195765-45-7
Dabrafenib/达拉非尼 3D分子结构 CAS号：1195765-45-7
规格 价格 会员价 库存 数量
{[ item.pr_size ]}

{[ getRatePriceInt(item.pr_rmb, 1,1) ]}

{[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}

{[ getRatePriceInt(item.pr_rmb, 1,1) ]}

{[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} 		{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]} 现货 1周 咨询 - +
购物车0 收藏 询单

Dabrafenib/达拉非尼 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]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
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, Kd: 36 nM

B-Raf (V600E), Kd: 14 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

 		98%
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/达拉非尼 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-RafV600E 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-RafV600E-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-RafV600E 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-RafV600E) 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/达拉非尼 细胞实验

Cell Line
Concentration Treated Time Description References
MKN74 cells 10μM 72 h Dabrafenib significantly inhibited invasion ability of MKN74 cells Oncogene. 2021 May;40(19):3422-3433.
BGC823 cells 10μM 24 h Dabrafenib significantly inhibited migration ability of BGC823 cells Oncogene. 2021 May;40(19):3422-3433.
MKN74 cells 10μM 48 h Dabrafenib significantly inhibited migration ability of MKN74 cells Oncogene. 2021 May;40(19):3422-3433.
BGC823 cells 10μM 48 h Dabrafenib significantly inhibited invasion ability of BGC823 cells Oncogene. 2021 May;40(19):3422-3433.
Primary murine melanoma cells from TBP mice 500 nM 10 days To evaluate the inhibitory effect of Dabrafenib on melanoma spheroids, results showed that Dabrafenib significantly reduced the volume of spheroids. Cancer Res. 2023 Jul 14;83(14):2328-2344.
BGC823 cells 10μM 48 h Dabrafenib significantly reduced the number of invaded BGC823 cells, indicating inhibition of cell invasion Oncogene. 2021 May;40(19):3422-3433.
MKN74 cells 10μM 72 h Dabrafenib significantly reduced the number of invaded MKN74 cells, indicating inhibition of cell invasion Oncogene. 2021 May;40(19):3422-3433.
BGC823 cells 10μM 24 h Dabrafenib significantly reduced the number of migrated BGC823 cells, indicating inhibition of cell migration Oncogene. 2021 May;40(19):3422-3433.
MKN74 cells 10μM 48 h Dabrafenib significantly reduced the number of migrated MKN74 cells, indicating inhibition of cell migration Oncogene. 2021 May;40(19):3422-3433.
BGC823 cells 10μM 72 h Dabrafenib significantly delayed wound closure in BGC823 cells, indicating inhibition of cell migration Oncogene. 2021 May;40(19):3422-3433.
MKN74 cells 10μM 72 h Dabrafenib significantly delayed wound closure in MKN74 cells, indicating inhibition of cell migration Oncogene. 2021 May;40(19):3422-3433.
BGC823 cells 10μM 72 h Dabrafenib significantly inhibited wound healing and migration ability of BGC823 cells Oncogene. 2021 May;40(19):3422-3433.
MKN74 cells 10μM 72 h Dabrafenib significantly inhibited wound healing and migration ability of MKN74 cells Oncogene. 2021 May;40(19):3422-3433.
inner ear cell line 30 nM Dabrafenib at a concentration of 30 nM protected neonatal mouse cochlear outer hair cells from cisplatin-induced cell death with a therapeutic index greater than 2000. JCI Insight. 2023 Dec 22;8(24):e171140.
A375 melanoma cells 1 μM 9 days or more To investigate the effect of Dabrafenib on A375 melanoma cells, results showed that these cells developed resistance to Dabrafenib treatment, but the resistance was reversible. Nature. 2017 Nov 9;551(7679):247-250.
MM200 cells 100 nM 24 h To assess the contribution of PI3K/AKT signaling in BRAF/MEK inhibitor resistance, results showed that PI3K/AKT activation promoted cell survival but did not restore MAPK signaling. Oncogenesis. 2018 Sep 20;7(9):72.
SKMel28 cells 100 nM 24 h To assess the contribution of PI3K/AKT signaling in BRAF/MEK inhibitor resistance, results showed that PI3K/AKT activation promoted cell survival but did not restore MAPK signaling. Oncogenesis. 2018 Sep 20;7(9):72.
WM164 cells 160 nM 72 h To assess the heterogeneity of MITF expression during BRAF inhibitor treatment, the results showed that MITF expression remained heterogeneous during treatment. EMBO Mol Med. 2017 Aug;9(8):1011-1029.

Dabrafenib/达拉非尼 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice TBP mouse melanoma model Oral 30 mg/kg Once daily for 5 weeks To evaluate the therapeutic effect of Dabrafenib on melanoma, results showed that Dabrafenib significantly reduced tumor volume, but eventually all tumors developed resistance. Cancer Res. 2023 Jul 14;83(14):2328-2344.
Nude mice Peritoneal metastasis model Intraperitoneal injection 5 mg/kg Every 3 days for 28 days Dabrafenib significantly reduced the number of peritoneal metastases, indicating inhibition of peritoneal metastasis Oncogene. 2021 May;40(19):3422-3433.
Nude mice Peritoneal metastasis model Intraperitoneal injection 5 mg/kg Every 3 days for 28 days Dabrafenib significantly inhibited peritoneal metastasis of MKN74 cells in nude mice Oncogene. 2021 May;40(19):3422-3433.
Mice Multidose cisplatin mouse model Oral 3 mg/kg Twice daily for 42 days Dabrafenib at a dose of 3 mg/kg BW, administered twice daily, significantly protected mice from cisplatin-induced hearing loss, and the protective effect persisted for 4 months after the completion of treatment. JCI Insight. 2023 Dec 22;8(24):e171140.
Nude mice A375 melanoma xenograft model Oral gavage 100 mg/kg Twice daily, until tumour relapse To investigate the effect of Dabrafenib on the A375 melanoma xenograft model, results showed that GPX4 KO tumours did not relapse after Dabrafenib treatment, while GPX4 WT tumours relapsed. Nature. 2017 Nov 9;551(7679):247-250.
Mice A375 tumor model Oral 25 mg/kg Once daily for 20 days To evaluate the effect of Dabrafenib combined with EDNR inhibitors on tumor growth, the results showed that combination therapy significantly inhibited tumor growth and reduced the number of AXL-high expressing cells. EMBO Mol Med. 2017 Aug;9(8):1011-1029.

Dabrafenib/达拉非尼 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.
Cmax 9.4 - 11.8 µg/ml
Tmax 0.5 - 1 h
AUC0→t 19.2 - 24.3 µg·h/ml

Dabrafenib/达拉非尼 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/达拉非尼 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/达拉非尼 技术信息

CAS号1195765-45-7
分子式C23H20F3N5O2S2
分子量 519.56
SMILES Code O=S(C1=C(F)C=CC=C1F)(NC2=CC=CC(C3=C(C4=NC(N)=NC=C4)SC(C(C)(C)C)=N3)=C2F)=O
MDL No. MFCD17215684
别名 达拉菲尼 ;GSK2118436A; GSK2118436
运输蓝冰
InChI Key BFSMGDJOXZAERB-UHFFFAOYSA-N
Pubchem ID 44462760
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, room temperature
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
方案 四
方案 五
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一
方案 二

Tags: Dabrafenib | GSK2118436A;GSK2118436 | 达拉菲尼 | Raf | AmBeed-信号通路专用抑制剂 | Dabrafenib/达拉非尼 纯度/质量文件 | Dabrafenib/达拉非尼 亚型比较 | Dabrafenib/达拉非尼 生物活性 | Dabrafenib/达拉非尼 动物研究 | Dabrafenib/达拉非尼 参考文献 | Dabrafenib/达拉非尼 实验方案 | Dabrafenib/达拉非尼 技术信息

AmBeed 相关网站 AmBeed.cn AmBeed.com
AmBeed
关于我们
联系我们
资讯中心
网站地图
产品手册
  • 批次文件查询
    • 客户支持
    技术支持
    专业术语
    缩略词释义
    质量手册
    产品咨询
    计算器
    活动政策
    订购方法
    积分商城
    活动声明
    联系我们
    400-920-2911 sales@ambeed.cn tech@ambeed.cn
    AmBeed 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质用途提供服务。

    尊敬的 AmBeed 客户您好，
    请您选择所在区域，我们将转接对应客服为您服务！

    热门区域

    A

    B

    C

    F

    G

    H

    J

    L

    N

    Q

    S

    T

    X

    Y

    Z

    热 A B C F G H J L N Q S T X Y Z