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  2. Protein Tyrosine Kinase/RTK
  3. TAM Receptor
  4. Bemcentinib

Bemcentinib (R428) 是一種選擇性的、具有口服活性的 Axl 抑制劑，IC50 值為 14 nM。

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Bemcentinib Chemical Structure

Bemcentinib Chemical Structure

CAS No. : 1037624-75-1

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1560
In-stock
2 mg ￥779
In-stock
5 mg ￥1400
In-stock
10 mg ￥2438
In-stock
50 mg ￥4700
In-stock
100 mg 現(xiàn)貨 詢價(jià)
200 mg   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Bemcentinib:

MCE 顧客使用本產(chǎn)品發(fā)表的 43 篇科研文獻(xiàn)

WB

    Bemcentinib purchased from MCE. Usage Cited in: Mil Med Res. 2023 Feb 22;10(1):7.  [Abstract]

    Bemcentinib (BGB324; 1 μM; 30 min) partially blocks the activation of HSC by rGAS6 in LX-2 cells.

    Bemcentinib purchased from MCE. Usage Cited in: Cancer Cell. 2018 Dec 10;34(6):954-969.e4.  [Abstract]

    Western blot showing PKCδ expression in nuclear extracts of GR4 and GR10 cells treated with 1 μM gef in combination with 2.5 μM R428 and 5 μM GW572016 (Lapa) for 24 hr.

    Bemcentinib purchased from MCE. Usage Cited in: Cancer Cell. 2018 Dec 10;34(6):954-969.e4.  [Abstract]

    Western blot showing phosphorylated PLCγ2 in cells treated with gef (1 μM) and R428 or Lapa for 24 hr. SE, short exposure; LE, long exposure.

    Bemcentinib purchased from MCE. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278.  [Abstract]

    BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 μM) or JuA (25 μM) with the indicated antagonist of TAM receptor (LDC1267 at 1 μM, UNC2250 at 5 μM, R428 at 5 μM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.

    Bemcentinib purchased from MCE. Usage Cited in: Sci Rep. 2017 Dec 19;7(1):17770.  [Abstract]

    Western blot analysis of pAXL level in H1299 cells treated with the indicated concentration of R428 for 1?h. Results are confirmed in three independent experiments.

    Bemcentinib purchased from MCE. Usage Cited in: Oncotarget. 2017 Jun 20;8(25):41064-41077.  [Abstract]

    The expression of AXL in the PC3-DR and DU145-DR cells treated with R428 (1 μM) is analyzed by western blotting.

    查看 TAM Receptor 亞型特異性產(chǎn)品:

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Bemcentinib (R428) is a potent and selective inhibitor of Axl with an IC50 of 14 nM[2].

    IC50 & Target

    Axl

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    4T1 IC50
    0.94 μM
    Compound: 1; R428, BGB-324
    Antiproliferative activity against mouse 4T1 cells highly expressing AXL after 72 hrs by MTT assay
    Antiproliferative activity against mouse 4T1 cells highly expressing AXL after 72 hrs by MTT assay
    		[PMID: 35279611]
    BaF3 IC50
    117.2 nM
    Compound: 8; R428; BGB324
    Antiproliferative activity against mouse BaF3 stably expressing human TEL-AXL incubated for 72 hrs
    Antiproliferative activity against mouse BaF3 stably expressing human TEL-AXL incubated for 72 hrs
    		[PMID: 33957388]
    GES1 IC50
    > 60 μM
    Compound: 1; R428, BGB-324
    Cytotoxicity against human GES1 cells after 72 hrs by MTT assay
    Cytotoxicity against human GES1 cells after 72 hrs by MTT assay
    		[PMID: 35279611]
    HeLa IC50
    < 30 nM
    Compound: 17; BGB324; R428
    Inhibition of recombinant AXL in human HeLa cells after 1 hr by ELISA
    Inhibition of recombinant AXL in human HeLa cells after 1 hr by ELISA
    		[PMID: 26555154]
    MCF-10A IC50
    > 60 μM
    Compound: 1; R428, BGB-324
    Cytotoxicity against human MCF-10A cells after 72 hrs by MTT assay
    Cytotoxicity against human MCF-10A cells after 72 hrs by MTT assay
    		[PMID: 35279611]
    MDA-MB-231 IC50
    2.84 μM
    Compound: 1; R428, BGB-324
    Antiproliferative activity against human MDA-MB-231 cells highly expressing AXL after 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells highly expressing AXL after 72 hrs by MTT assay
    		[PMID: 35279611]
    體外研究
    (In Vitro)

    Bemcentinib (R428) (2 μM) 顯著干擾Axlpos黑色素瘤細(xì)胞的遷移和侵襲機(jī)制，其水平與Axl敲低相當(dāng)[1]。bmcentinib (R428)協(xié)同CDDP增強(qiáng)肝臟微轉(zhuǎn)移抑制作用[2]。
    bmcentinib (R428) (50 nM-1 μM)可引起前脂肪細(xì)胞向成熟脂肪細(xì)胞分化的濃度依賴性抑制，這可以通過降低脂質(zhì)攝取得到證明[3]。

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

    Bemcentinib (R428) (125 mg/kg, p.o.) 顯著阻斷MDA-MB-231-luc-D3H2LN在兩種獨(dú)立小鼠乳腺癌擴(kuò)散模型中的轉(zhuǎn)移發(fā)展，抑制腫瘤血管生成和血管內(nèi)皮生長因子(VEGF)誘導(dǎo)的角膜新生血管生成[2].
    Bemcentinib (R428) (75 mg/kg/day, 25 mg/kg twice daily, p.o.) 讓老鼠保持高脂肪飲食導(dǎo)致體重增加和皮下和性腺脂肪量顯著減少[3]。

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

    506.64

    Formula

    C30H34N8
    CAS 號
    性狀

    固體

    顏色

    Off-white to yellow

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 12.5 mg/mL (24.67 mM; 超聲助溶 (<60°C); 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)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 1.9738 mL 9.8689 mL 19.7379 mL
    5 mM 0.3948 mL 1.9738 mL 3.9476 mL
    查看完整儲(chǔ)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(chǔ)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(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)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(dòng)物實(shí)驗(yàn)：

    請根據(jù)您的 實(shí)驗(yàn)動(dòng)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(chǔ)備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (4.11 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.08 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)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： 0.5% CMC-Na/saline water

      Solubility: 12.5 mg/mL (24.67 mM); 懸濁液; 超聲助溶

    • 方案 二

      請依序添加每種溶劑： 0.5% HPMC/1% Tween-80 in Saline water

      Solubility: 5 mg/mL (9.87 mM); 懸濁液; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
    請輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)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(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)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(chǔ)備液濃度超過該產(chǎn)品的實(shí)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(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)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(chǔ)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: 99.92%

    參考文獻(xiàn)
    Cell Assay
    [1]

    Cells maintained for 24 hours in serum-free medium are harvested and transferred to the upper chamber (1.5×105 cells per well) of uncoated (migration) or matrigel-coated (invasion) 24-well chambers. RPMI medium containing 10% fetal bovine serum is added to the lower chamber. Bemcentinib (R428) (2 μM) or vehicle (DMSO, 0.25%) is added for 2 hours to cells before loading them in the upper chambers. Both the upper and lower chambers contain the drug or vehicle. Quantification of migrating/invading cells is obtained by measuring their fluorescent signals with a 480/520 nm filter set on an Infinite M1000 microplate reader 20 or 42 hours later, respectively.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Seven- to 8-wk-old female NCr?nu/nu?mice are injected intracardially with bioluminescent MDA-MB-231-luc-D3H2LN cell suspension. Oral dosing with Bemcentinib (R428) (125 mg/kg, p.o.) or vehicle twice daily begins 2 h before cell implantation and continue to day 21 (n=20). Metastatic burden is quantified by?in vivo bioluminescence imaging on day 22 and analyzed using the Wilcoxon rank sum test.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    參考文獻(xiàn)

    完整儲(chǔ)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(chǔ)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(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(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 1.9738 mL 9.8689 mL 19.7379 mL 49.3447 mL
    5 mM 0.3948 mL 1.9738 mL 3.9476 mL 9.8689 mL
    10 mM 0.1974 mL 0.9869 mL 1.9738 mL 4.9345 mL
    15 mM 0.1316 mL 0.6579 mL 1.3159 mL 3.2896 mL
    20 mM 0.0987 mL 0.4934 mL 0.9869 mL 2.4672 mL
    Help & FAQs
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      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：
    Bemcentinib
    目錄號：
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