2. MAPK/ERK Pathway
  3. Raf
  4. Dabrafenib

Dabrafenib  (Synonyms: 达拉非尼; GSK2118436A; GSK2118436)

目录号: HY-14660 纯度: 99.94%
COA 产品使用指南 技术支持

Dabrafenib (GSK2118436A) 是ATP竞争型的 Raf 抑制剂，抑制 C-Raf 和 B-RafV600E 的 IC50 分别为 5 nM 和 0.6 nM。

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Dabrafenib Chemical Structure

Dabrafenib Chemical Structure

CAS No. : 1195765-45-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥743
In-stock
5 mg ￥650
In-stock
10 mg ￥850
In-stock
50 mg ￥1900
In-stock
100 mg ￥2900
In-stock
200 mg ￥4900
In-stock
500 mg 现货 询价
1 g 现货 询价
5 g   询价  
10 g   询价  

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Customer Review

Other Forms of Dabrafenib:

Dabrafenib 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 56 篇科研文献

WB

    Dabrafenib purchased from MCE. Usage Cited in: Int J Cancer. 2019 Mar 15;144(6):1379-1390.  [Abstract]

    Western blot confirmed increased MAPK pathway activity in NEC-DUE2 cells when compared to NECDUE1. Treatment with PLX4032 (1 μM), Dabrafenib (100 nM), or GSK1120212 (100 nM) for 4 hours leads to decreased MAPK signaling in NEC-DUE2 cells. Lysates are immunoblotted for the proteins indicated.

    查看 Raf 亚型特异性产品:

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    BRaf c-Raf Raf

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively[4].

    IC50 & Target[4]

    BRafV600E

    0.6 nM (IC50)

    CRAF

    5 nM (IC50)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A-375 IC50
    0.011 μM
    Compound: 2
    Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay
    Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay
    		[PMID: 25965804]
    A-375 IC50
    0.457 nM
    Compound: DB
    Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth measured after 5 days by MTT assay
    Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth measured after 5 days by MTT assay
    		[PMID: 34958586]
    A-375 IC50
    1 nM
    Compound: 3
    Inhibition of B-Raf V600E mutant in human A375 cells assessed as ERK phosphorylation preincubated for 1 hr by Western blot method
    Inhibition of B-Raf V600E mutant in human A375 cells assessed as ERK phosphorylation preincubated for 1 hr by Western blot method
    		[PMID: 27085672]
    A-375 IC50
    150 nM
    Compound: 2
    Competitive binding affinity to CRAF in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to CRAF in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 IC50
    26 nM
    Compound: 2
    Competitive binding affinity to ARAF in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to ARAF in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 IC50
    6 nM
    Compound: 2
    Competitive binding affinity to BRAF in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to BRAF in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    HCT-116 IC50
    5.88 μM
    Compound: 2
    Inhibition of KRAS G13D mutant in human HCT116 cells assessed as inhibition of ERK phosphorylation by ELISA
    Inhibition of KRAS G13D mutant in human HCT116 cells assessed as inhibition of ERK phosphorylation by ELISA
    		[PMID: 25965804]
    HepG2 IC50
    3.7 μM
    Compound: 12, GSK2118436, Dabrafenib
    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
    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
    		[PMID: 24900673]
    MIA PaCa-2 EC50
    529 nM
    Compound: 3
    Inhibition of wild type B-Raf in human MIAPaCa2 cells assessed as reduction in ERK phosphorylation preincubated for 1 hr by Western blot method
    Inhibition of wild type B-Raf in human MIAPaCa2 cells assessed as reduction in ERK phosphorylation preincubated for 1 hr by Western blot method
    		[PMID: 27085672]
    Sf9 IC50
    250 nM
    Compound: 58
    Inhibition of human full length N-terminal GST-tagged RIPK3 expressed in baculovirus infected sf9 insect cells assessed as reduction in MBP phosphorylation using MBP as substrate by kinase-Glo luminescence assay
    Inhibition of human full length N-terminal GST-tagged RIPK3 expressed in baculovirus infected sf9 insect cells assessed as reduction in MBP phosphorylation using MBP as substrate by kinase-Glo luminescence assay
    		[PMID: 31622096]
    Sf9 IC50
    9 nM
    Compound: 1
    Inhibition of recombinant human N-terminal GST-6His tagged BRAF V600E mutant (417 to 766 residues) expressed in baculovirus infected Sf9 cells preincubated with substrate followed by protein and ATP addition measured after 60 mins by scintillation counter
    Inhibition of recombinant human N-terminal GST-6His tagged BRAF V600E mutant (417 to 766 residues) expressed in baculovirus infected Sf9 cells preincubated with substrate followed by protein and ATP addition measured after 60 mins by scintillation counter
    		[PMID: 27774137]
    SK-MEL-28 IC50
    3 nM
    Compound: 12, GSK2118436, Dabrafenib
    Inhibition of B-Raf V600E mutant-driven SK-MEL-28 cell proliferation after 72 hrs by CellTiter-Glo luminescent assay
    Inhibition of B-Raf V600E mutant-driven SK-MEL-28 cell proliferation after 72 hrs by CellTiter-Glo luminescent assay
    		[PMID: 24900673]
    SK-MEL-28 IC50
    4 nM
    Compound: 12, GSK2118436, Dabrafenib
    Inhibition of B-Raf V600E mutant in human SK-MEL-28 cells assessed as decrease in ERK phosphorylation incubated for 1 hr by immunoassay
    Inhibition of B-Raf V600E mutant in human SK-MEL-28 cells assessed as decrease in ERK phosphorylation incubated for 1 hr by immunoassay
    		[PMID: 24900673]
    SK-MEL-28 IC50
    43 nM
    Compound: 6
    Cytotoxicity against human SK-MEL-28 cells after 72 hrs by CellTiter-Glo assay
    Cytotoxicity against human SK-MEL-28 cells after 72 hrs by CellTiter-Glo assay
    		[PMID: 29461827]
    体外研究
    (In Vitro)

    Dabrafenib (GSK2118436，1 μM) 与 0.01 μM GSK1120212 结合可抑制 NRAS 突变克隆中 90% 以上的细胞生长。Dabrafenib 足以降低 A375[1] 中的 S6P 磷酸化。Dabrafenib 可抑制 PolyP 介导的血管屏障通透性、炎症生物标志物的上调、白细胞的粘附/迁移以及NF-κB、TNF-α 和 IL-6 的激活和/或产生[2]。Dabrafenib 通过增强人内皮细胞中细胞粘附分子 (CAM) 的表达来抑制 HMGB1 的释放并下调 HMGB1 依赖性炎症反应[3]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Dabrafenib 相关抗体:
    体内研究
    (In Vivo)

    与年龄匹配的对照组相似，接受 Dabrafenib 治疗的雌性大多数生殖道尚未成熟，且没有排卵的迹象；然而，接受 Dabrafenib 治疗的雌性阴道角化且组织学上开放[5]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    分子量

    519.56

    Formula

    C23H20F3N5O2S2
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    达拉非尼；达拉菲尼
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 33 mg/mL (63.52 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.9247 mL 9.6235 mL 19.2471 mL
    5 mM 0.3849 mL 1.9247 mL 3.8494 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制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

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.81 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.81 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

    以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制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

      请依序添加每种溶剂： 30% PEG400    0.5% Tween-80    5% Propanediol    64.5% H2O

      Solubility: 5 mg/mL (9.62 mM); 悬浊液; 超声助溶

    • 方案 二

      请依序添加每种溶剂： 0.5% HPMC in Water

      Solubility: 2.5 mg/mL (4.81 mM); 悬浊液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.94%

    COA (296 KB) HNMR (268 KB) RP-HPLC (244 KB) LCMS (105 KB) 元素分析报告 (220 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [1]

    For longer term proliferation assays, cells are plated and treated with compound or combination of compounds in RMPI-1640 containing 10% FBS for 12 days. Compound treatments are replaced at least once during the assay. After 12 days, cells are stained with 0.5% methylene blue in 50% ethanol. Images are captured using flatbed scanner.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [5]

    The rat pups selected as the test system are derived from 26 10-week-old, time-mated, virus-antibody-free SD (Crl:CD[SD]) female rats. Mated females are observed for natural deliveries from Day 20 to 23 pc (day parturition completed is designated PND 0). Litter examinations are conducted when parturition is complete, on PNDs 3 and 6, and included gender identification, individual pup weights, and external morphologic examinations. Parturient dams and their litters are selected for study based on clinical signs and body weights, and selected dams and their litters are randomized into study groups based on clinical observations and PND 3 litter mean body weights. On PND 3 or 4, litters are culled to four males and five females, with minimal fostering only when necessary to obtain the desired sex ratio, such that natural litters are maintained as much as possible. Records are kept of fostered pups of original and foster dams. All pups are identified by paw tattoo. To the extent possible, nonlittermates are assigned to subsets. DAB is formulated as a suspension in vehicle, 0.5% hydroxypropylmethylcellulose K15M, and 0.1% (v/v) Tween80 in purified water, and is given to juvenile male and female rats orally by gavage at a dose volume of 5 ml/kg, based on daily body weight.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    Dabrafenib 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9247 mL 9.6235 mL 19.2471 mL 48.1176 mL
    5 mM 0.3849 mL 1.9247 mL 3.8494 mL 9.6235 mL
    10 mM 0.1925 mL 0.9624 mL 1.9247 mL 4.8118 mL
    15 mM 0.1283 mL 0.6416 mL 1.2831 mL 3.2078 mL
    20 mM 0.0962 mL 0.4812 mL 0.9624 mL 2.4059 mL
    25 mM 0.0770 mL 0.3849 mL 0.7699 mL 1.9247 mL
    30 mM 0.0642 mL 0.3208 mL 0.6416 mL 1.6039 mL
    40 mM 0.0481 mL 0.2406 mL 0.4812 mL 1.2029 mL
    50 mM 0.0385 mL 0.1925 mL 0.3849 mL 0.9624 mL
    60 mM 0.0321 mL 0.1604 mL 0.3208 mL 0.8020 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Dabrafenib1195765-45-7GSK2118436A GSK2118436达拉非尼达拉菲尼GSK2118436GSK 2118436GSK-2118436RafRaf kinasesInhibitorinhibitorinhibit

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