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  2. Protein Tyrosine Kinase/RTK Apoptosis
  3. Syk FLT3 Apoptosis
  4. R406 free base

R406 free base 是一種有效的，具有口服活性的，ATP競爭性的 Syk/FLT3 抑制劑，Ki 為 30 nM，有效抑制 Syk 激酶活性，IC50 為 41 nM。R406 free base 可減輕免疫復合物介導的炎癥。R406 free base 還抑制 Lyn (IC50=63 nM) 和 Lck (IC50=37 nM).

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R406 free base Chemical Structure

R406 free base Chemical Structure

CAS No. : 841290-80-0

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥828
In-stock
1 mg ￥500
In-stock
5 mg ￥800
In-stock
10 mg ￥1300
In-stock
50 mg ￥4300
In-stock
100 mg 現(xiàn)貨 詢價
200 mg   詢價  
500 mg   詢價  

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Customer Review

Other Forms of R406 free base:

    R406 free base purchased from MCE. Usage Cited in: Cell. 2018 Oct 4;175(2):442-457.e23.  [Abstract]

    Syk inhibitors (R406 and Piceatannol) are added during the induction of trastuzumab-dependent BT-474 phagocytosis. The binding of the phagosome marker Rab7 to AIM2 in macrophages are evaluated by co-immunoprecipitation.

    R406 free base purchased from MCE. Usage Cited in: J Pharmacol Sci. 2017 May;134(1):29-36.  [Abstract]

    The effects of R406 treatment on the phosphorylation of 3BP2 and p38MAPK in white blood cells from the spleens of NZB/W F1 mice. (A) The phosphorylation of the 3BP2 and (B) the phosphorylation of p38MAPK in the renal cortex of control and R406-treated mice.

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 free base reduces immune complex-mediated inflammation[1]. R406 free base also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM)[2].

    IC50 & Target

    Ki: 30 nM (Syk)[1]
    IC50: 41 nM (Syk)[1]
    FLT3[1]
    IC50: 63 nM (Lyn), 37 nM (Lck)[2]
    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    Bone marrow cell IC50
    147 nM
    Compound: 2
    Inhibition of IL3 dependent proliferation in C57/B16 mouse bone marrow cells using [3H]thymidine by liquid scintillation counting
    Inhibition of IL3 dependent proliferation in C57/B16 mouse bone marrow cells using [3H]thymidine by liquid scintillation counting
    		[PMID: 24726806]
    HUVEC EC50
    36 nM
    Compound: 1, R406
    Inhibition of KDR in VEGF-stimulated HUVEC assessed as phosphorylation after 1 hr incubation
    Inhibition of KDR in VEGF-stimulated HUVEC assessed as phosphorylation after 1 hr incubation
    		[PMID: 24779514]
    MV4-11 EC50
    10 nM
    Compound: 1, R406
    Inhibition of Flt3 in human MV411 cells assessed as assessed as proliferation after 72 hrs incubation by spectrophotometry
    Inhibition of Flt3 in human MV411 cells assessed as assessed as proliferation after 72 hrs incubation by spectrophotometry
    		[PMID: 24779514]
    Ramos IC50
    457 nM
    Compound: 2
    Inhibition of Syk in anti IgM-stimulated human Ramos cells assessed as BLNK phosphorylation by cellular assay
    Inhibition of Syk in anti IgM-stimulated human Ramos cells assessed as BLNK phosphorylation by cellular assay
    		[PMID: 24726806]
    Ramos EC50
    53 nM
    Compound: 1, R406
    Inhibition of Syk in antihuman IgM-stimulated human Ramos cells assessed as decrease in BCR-mediated BLNK phosphorylation by cellular assay
    Inhibition of Syk in antihuman IgM-stimulated human Ramos cells assessed as decrease in BCR-mediated BLNK phosphorylation by cellular assay
    		[PMID: 24779514]
    TF-1 EC50
    13 nM
    Compound: 1, R406
    Inhibition of Jak2 in erythropoietin-stimulated human TF1 cells assessed as assessed as phospho-Stat5 after 1 hr incubation
    Inhibition of Jak2 in erythropoietin-stimulated human TF1 cells assessed as assessed as phospho-Stat5 after 1 hr incubation
    		[PMID: 24779514]
    體外研究
    (In Vitro)

    R406 inhibits adenosine A3 receptor (IC50=0.081 μM), adenosine transporter (IC50=1.84 μM), and monoamine transporter (IC50=2.74 μM)[1].
    R406 inhibits Huh7 hepatocyte, A549 epithelial, and H1299 lung cancer lines with EC50s of 15.1, 2.9 and 6.3 μM, respectively[1].
    R406 inhibits phosphorylation of Syk substrate LAT in mast cells and BLNK/SLP65 in B cells[1].

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

    Western Blot Analysis[1]

    Cell Line: Cultured human mast cells (CHMC)
    Concentration: 0.016, 0.08, 0.4, 2 μM
    Incubation Time: 40 minutes
    Result: Inhibited all other kinases tested at 5 to 100 fold less potency than Syk as judged by phosphorylation of target proteins.
    體內研究
    (In Vivo)

    R406 (5 and 10 mg/kg) shows efficacy in the amelioration of the Arthus reaction and in reducing clinical symptoms in the collagen antibody-induced arthritis (CAIA) and K/BxN models of rheumatoid arthritis (RA). Immune complex (IC)-mediated inflammation is reduced by inhibition of Fc receptor signaling with R406[1].

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

    Animal Model: Female Balb/c mice (6-8 weeks) with CAIA[1]
    Dosage: 5 and 10 mg/kg
    Administration: Administered orally, b.i.d, for 14 days, starting 4 hours after antibody challenge on day 0.
    Result: Reduced inflammation and swelling, and the arthritis progressed more slowly in treated animals than in vehicle controls.
    Animal Model: Female C57BL/6 mice with arthritis[1]
    Dosage: 10 mg/kg
    Administration: Administered orally one hour before serum injection; b.i.d; for 13 days
    Result: Delayed the onset and reduced the severity of clinical arthritis. Paw thickening and clinical arthritis were reduced by approximately 50%.
    分子量

    470.45

    Formula

    C22H23FN6O5
    CAS 號
    性狀

    固體

    顏色

    White to light yellow

    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)
    細胞實驗： 

    DMSO 中的溶解度 : 25 mg/mL (53.14 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)

    配制儲備液
    濃度 溶劑體積 質量 1 mg 5 mg 10 mg
    1 mM 2.1256 mL 10.6281 mL 21.2562 mL
    5 mM 0.4251 mL 2.1256 mL 4.2512 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年內使用， -20°C儲存時，請在1年內使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質量
    =
    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?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：
    ——為保證實驗結果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
    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 (5.31 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.5 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 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.31 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，此方案實驗周期在半個月以上的動物實驗酌情使用。

      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玉米油中，混合均勻。

    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 中國技術支持聯(lián)系。
    動物實驗體內工作液的配制方法 : 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: 99.80%

    參考文獻

    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年內使用， -20°C儲存時，請在1年內使用。

    可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1256 mL 10.6281 mL 21.2562 mL 53.1406 mL
    5 mM 0.4251 mL 2.1256 mL 4.2512 mL 10.6281 mL
    10 mM 0.2126 mL 1.0628 mL 2.1256 mL 5.3141 mL
    15 mM 0.1417 mL 0.7085 mL 1.4171 mL 3.5427 mL
    20 mM 0.1063 mL 0.5314 mL 1.0628 mL 2.6570 mL
    25 mM 0.0850 mL 0.4251 mL 0.8502 mL 2.1256 mL
    30 mM 0.0709 mL 0.3543 mL 0.7085 mL 1.7714 mL
    40 mM 0.0531 mL 0.2657 mL 0.5314 mL 1.3285 mL
    50 mM 0.0425 mL 0.2126 mL 0.4251 mL 1.0628 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：
    R406 free base
    目錄號：
    HY-11108
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