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

Dabrafenib  (Synonyms: 達(dá)拉非尼; GSK2118436A; GSK2118436)

目錄號: HY-14660 純度: 99.94%
COA 產(chǎn)品使用指南 技術(shù)支持

Dabrafenib (GSK2118436A) 是ATP競爭型的 Raf 抑制劑，抑制 C-Raf 和 B-RafV600E 的 IC50 分別為 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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規(guī)格 價格 是否有貨 數(shù)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 現(xiàn)貨 詢價
1 g 現(xiàn)貨 詢價
5 g   詢價  
10 g   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Dabrafenib:

MCE 顧客使用本產(chǎn)品發(fā)表的 58 篇科研文獻(xiàn)

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 亞型特異性產(chǎn)品:

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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)

    細(xì)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]
    體外研究
    (In Vitro)

    Dabrafenib (GSK2118436，1 μM) 與 0.01 μM GSK1120212 結(jié)合可抑制 NRAS 突變克隆中 90% 以上的細(xì)胞生長。Dabrafenib 足以降低 A375[1] 中的 S6P 磷酸化。Dabrafenib 可抑制 PolyP 介導(dǎo)的血管屏障通透性、炎癥生物標(biāo)志物的上調(diào)、白細(xì)胞的粘附/遷移以及NF-κB、TNF-α 和 IL-6 的激活和/或產(chǎn)生[2]。Dabrafenib 通過增強人內(nèi)皮細(xì)胞中細(xì)胞粘附分子 (CAM) 的表達(dá)來抑制 HMGB1 的釋放并下調(diào) HMGB1 依賴性炎癥反應(yīng)[3]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    與年齡匹配的對照組相似，接受 Dabrafenib 治療的雌性大多數(shù)生殖道尚未成熟，且沒有排卵的跡象；然而，接受 Dabrafenib 治療的雌性陰道角化且組織學(xué)上開放[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 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    達(dá)拉非尼；達(dá)拉菲尼
    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實驗： 

    DMSO 中的溶解度 : ≥ 33 mg/mL (63.52 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

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

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

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

    以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請依序添加每種溶劑： 30% PEG400    0.5% Tween-80    5% Propanediol    64.5% H2O

      Solubility: 5 mg/mL (9.62 mM); 懸濁液; 超聲助溶

    • 方案 二

      請依序添加每種溶劑： 0.5% HPMC in Water

      Solubility: 2.5 mg/mL (4.81 mM); 懸濁液; 超聲助溶

    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.94%

    參考文獻(xiàn)
    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.
    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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.

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    產(chǎn)品名稱：
    Dabrafenib
    目錄號：
    HY-14660
    需求量：