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  1. Protein Tyrosine Kinase/RTK
  2. Btk BMX Kinase
  3. BMX-IN-1

BMX-IN-1  (Synonyms: BMX kinase inhibitor)

目錄號(hào): HY-80002 純度: 98.90%
COA 產(chǎn)品使用指南 技術(shù)支持

BMX-IN-1 是一種選擇性、不可逆的 X 染色體上骨髓酪氨酸激酶 (BMX) 抑制劑,靶向 BMX ATP 結(jié)合域中的 Cys496,IC50 為 8 nM,還靶向相關(guān)的布魯頓酪氨酸激酶 (BTK),具有 IC50 值為 10.4 nM,但對(duì) Blk、JAK3、EGFR、Itk 或 Tec 活性的效力低 47-656 倍以上。

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BMX-IN-1 Chemical Structure

BMX-IN-1 Chemical Structure

CAS No. : 1431525-23-3

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10 mM * 1 mL in DMSO ¥1812
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1 mg ¥616
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5 mg ¥1570
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10 mg ¥2520
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25 mg ¥5000
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    BMX-IN-1 purchased from MCE. Usage Cited in: Oncotarget. 2017 Jul 25;8(30):49238-49252.  [Abstract]

    Western blot results show that the expression of BMX is decreased in both BMX-IN-1-treated HeLa and SiHa cells.
    • 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

    BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.

    IC50 & Target

    IC50: 8 nM (BMX), 10.4 nM (BTK)

    體外研究
    (In Vitro)

    BMX-IN-1 抑制 Tel-BMX 轉(zhuǎn)化的 Ba/F3 細(xì)胞和 RV-1 細(xì)胞的增殖,IC50 分別為 25 nM 和 2.53 μM。BMX-IN-1 表現(xiàn)出顯著的選擇性,S (10) 得分為 0.01。BMX-IN-1 僅抑制野生型 BMX,IC50 為 138 nM。BMX-IN-1 需要對(duì) BMX 的 Cys496 進(jìn)行共價(jià)修飾才能實(shí)現(xiàn)有效抑制[1]。

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

    分子量

    524.59

    Formula

    C29H24N4O4S

    CAS 號(hào)
    性狀

    固體

    顏色

    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 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    DMF 中的溶解度 : 10 mg/mL (19.06 mM; 超聲助溶)

    DMSO 中的溶解度 : 8.33 mg/mL (15.88 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開(kāi)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 1.9063 mL 9.5313 mL 19.0625 mL
    5 mM 0.3813 mL 1.9063 mL 3.8125 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)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(qǐng)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, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(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):

    以下溶解方案,請(qǐng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑: 50% PEG300    50% Saline

      Solubility: 10 mg/mL (19.06 mM); 懸濁液; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)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

    由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    純度 & 產(chǎn)品資料

    純度: 99.04%

    參考文獻(xiàn)
    Cell Assay
    [1]

    RV-1 cells in complete or serum-reduced DMEM are treated with DMSO, BMX-IN-1 (2.5 μM), MK2206 (200 nM), or the combination of BMX-IN-1 and MK2206 for 5 days before cells are harvested by trypsin and washed with cold PBS. The cells are then fixed in 70% cold ethanol (prechilled at ?20°C) and incubated at 4°C overnight. On the day of flow cytometry, cells are collected by centrifugation, washed with PBS, and stained in 50 μg/mL propidium iodide + 0.5 mg/mL?RNase in PBS + 0.5% Triton-X100 for 30 min at RT and moved to 4°C until the time of analysis. Flow cytometry is performed using a BD FACScan, and results are analyzed by ModFit software in the Flow Cytometry Core Facility in Dana-Faber Cancer Institute.

    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(qǐng)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(qǐng)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, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?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 / DMF 1 mM 1.9063 mL 9.5313 mL 19.0625 mL 47.6563 mL
    5 mM 0.3813 mL 1.9063 mL 3.8125 mL 9.5313 mL
    10 mM 0.1906 mL 0.9531 mL 1.9063 mL 4.7656 mL
    15 mM 0.1271 mL 0.6354 mL 1.2708 mL 3.1771 mL
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    產(chǎn)品名稱(chēng):
    BMX-IN-1
    目錄號(hào):
    HY-80002
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