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  2. JAK/STAT Signaling Stem Cell/Wnt
  3. STAT
  4. BP-1-102

BP-1-102 是有口服活性的轉(zhuǎn)錄因子 Stat3 的小分子抑制劑，其 IC50 值為 6.8 μM。

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BP-1-102 Chemical Structure

BP-1-102 Chemical Structure

CAS No. : 1334493-07-0

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1310
In-stock
5 mg ￥950
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10 mg ￥1500
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50 mg ￥4500
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100 mg   詢價(jià)  
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Customer Review

    BP-1-102 purchased from MCE. Usage Cited in: Cell Commun Signal. 2020 Jul 8;18(1):104.  [Abstract]

    Immunoblotting analysis of pulmonary STAT3 and pY-STAT3 in mice 24?h after CLP with BP-1-102 (BP) administration. BP downregulates the elevated pY-STAT3 level in the mouse lung 24?h after CLP.

    查看 STAT 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

    BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3, with an IC50 of 6.8 μM.

    IC50 & Target[1]

    STAT3

    6.8 μM (IC50)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    143B IC50
    4.17 μM
    Compound: 1d; BP-1-102
    Antimigratory activity against human 143B cells assessed as reduction in cell migration measured after 12 hrs by wound healing assay
    Antimigratory activity against human 143B cells assessed as reduction in cell migration measured after 12 hrs by wound healing assay
    		[PMID: 35476936]
    143B IC50
    4.4 μM
    Compound: 1d; BP-1-102
    Antiinvasive activity against human 143B cells assessed as reduction in cell invasion measured after 12 hrs by crystal violet staining based inverted microscopic analysis
    Antiinvasive activity against human 143B cells assessed as reduction in cell invasion measured after 12 hrs by crystal violet staining based inverted microscopic analysis
    		[PMID: 35476936]
    143B IC50
    5.87 μM
    Compound: 1d; BP-1-102
    Antiproliferative activity against human 143B cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    Antiproliferative activity against human 143B cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    		[PMID: 35476936]
    DU-145 EC50
    22.7 μM
    Compound: 17o
    Cytotoxicity against human DU145 cells after 72 hrs by MTS assay
    Cytotoxicity against human DU145 cells after 72 hrs by MTS assay
    		[PMID: 21788134]
    DU-145 IC50
    23 μM
    Compound: 9, BP-1-102
    Cytotoxicity against human DU145 cells assessed as cell viability after 72 hrs by MTS assay
    Cytotoxicity against human DU145 cells assessed as cell viability after 72 hrs by MTS assay
    		[PMID: 23968501]
    HCT-116 IC50
    15.05 μM
    Compound: BP-1-102; 36
    Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
    		[PMID: 29674294]
    HOS IC50
    6.44 μM
    Compound: 1d; BP-1-102
    Antiproliferative activity against human HOS cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    Antiproliferative activity against human HOS cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    		[PMID: 35476936]
    JJN-3 EC50
    16.7 μM
    Compound: 17o
    Cytotoxicity against human JJN-3 cells after 72 hrs by MTS assay
    Cytotoxicity against human JJN-3 cells after 72 hrs by MTS assay
    		[PMID: 21788134]
    MDA-MB-231 IC50
    6.8 μM
    Compound: 14; BP-1-102
    Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay
    		[PMID: 28245116]
    MDA-MB-468 EC50
    10.9 μM
    Compound: 17o
    Cytotoxicity against human MDA468 cells after 72 hrs by MTS assay
    Cytotoxicity against human MDA468 cells after 72 hrs by MTS assay
    		[PMID: 21788134]
    MDA-MB-468 IC50
    11 μM
    Compound: 9, BP-1-102
    Cytotoxicity against human MDA468 cells assessed as cell viability after 72 hrs by MTS assay
    Cytotoxicity against human MDA468 cells assessed as cell viability after 72 hrs by MTS assay
    		[PMID: 23968501]
    MG-63 IC50
    12.66 μM
    Compound: 1d; BP-1-102
    Antiproliferative activity against human MG-63 cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    Antiproliferative activity against human MG-63 cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    		[PMID: 35476936]
    OCI-AML2 IC50
    10 μM
    Compound: 9, BP-1-102
    Cytotoxicity against human OCI-AML2 cells assessed as cell viability after 72 hrs by MTS assay
    Cytotoxicity against human OCI-AML2 cells assessed as cell viability after 72 hrs by MTS assay
    		[PMID: 23968501]
    U2OS IC50
    8.3 μM
    Compound: 14; BP-1-102
    Antiproliferative activity against human U2OS cells after 24 hrs by MTT assay
    Antiproliferative activity against human U2OS cells after 24 hrs by MTT assay
    		[PMID: 28245116]
    體外研究
    (In Vitro)

    BP-1-102 binds Stat3 with an affinity KD of 504 nM. BP-1-102 inhibits Stat3 DNA-binding activity in vitro, with an IC50 value of 6.8±0.8 μM. It blocks Stat3-phospho-tyrosine peptide interactions and Stat3 activation at 4-6.8 μM, and selectively inhibits growth, survival, migration, and invasion of Stat3-dependent tumor cells. BP-1-102-mediated inhibition of aberrantly active Stat3 in tumor cells suppresses the expression of c-Myc, Cyclin D1, Bcl-xL, Survivin, VEGF, and Krüppel-like factor 8[1].

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

    Mice therapeutically given BP-1-102, an orally bioavailable compound targeting STAT3/NF-kB activation and cross-talk, exhibit reduced colon tumorigenesis and diminished expression of STAT3/NF-kB-activating cytokines in the neoplastic areas[2]. BP-1-102 is orally bioavailable and that the agent accumulates in tumor tissues at levels sufficient to inhibit aberrantly active Stat3 functions and inhibit tumor growth[1].

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

    626.59

    Formula

    C29H27F5N2O6S
    CAS 號
    性狀

    固體

    顏色

    White to off-white

    運(yùn)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(shí)驗(yàn)： 

    DMSO 中的溶解度 : ≥ 33 mg/mL (52.67 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 1.5959 mL 7.9797 mL 15.9594 mL
    5 mM 0.3192 mL 1.5959 mL 3.1919 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(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，請?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

    動物實(shí)驗(yàn)：

    請根據(jù)您的 實(shí)驗(yàn)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(shí)驗(yàn)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(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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (3.99 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (3.99 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(shí)驗(yàn)周期在半個月以上的動物實(shí)驗(yàn)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(jì)算器
    請輸入動物實(shí)驗(yàn)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(shí)驗(yàn)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(jì)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(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。
    動物實(shí)驗(yàn)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
    參考文獻(xiàn)
    Cell Assay
    [1]

    Proliferating cells in 6- or 96-well plates are treated once with 0-30 μM BP-1-102 for 24 h or with 10 μM BP-1-102 for up to 96 h. Viable cells are counted by trypan blue exclusion/phase-contrast microscopy or assessed by a cell proliferation kit[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice: Athymic nude mice with established tumors are grouped and then given BP-1-102 (in 0.05% DMSO in water) at 1 or 3mg/kg (i.v.) every 2 or every 3 d or 3 mg/kg (oral gavage, 100 μL) every day for 15 or 20 d. Animals are monitored every day, and tumor sizes are measured with calipers and body weights are taken every 2 or 3 d. For each treatment group, the tumor volumes for each set of measurements are statistically analyzed in comparison with the control group using a paired T test[1].

    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(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，請?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 1 mM 1.5959 mL 7.9797 mL 15.9594 mL 39.8985 mL
    5 mM 0.3192 mL 1.5959 mL 3.1919 mL 7.9797 mL
    10 mM 0.1596 mL 0.7980 mL 1.5959 mL 3.9898 mL
    15 mM 0.1064 mL 0.5320 mL 1.0640 mL 2.6599 mL
    20 mM 0.0798 mL 0.3990 mL 0.7980 mL 1.9949 mL
    25 mM 0.0638 mL 0.3192 mL 0.6384 mL 1.5959 mL
    30 mM 0.0532 mL 0.2660 mL 0.5320 mL 1.3299 mL
    40 mM 0.0399 mL 0.1995 mL 0.3990 mL 0.9975 mL
    50 mM 0.0319 mL 0.1596 mL 0.3192 mL 0.7980 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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    Inquiry Information

    產(chǎn)品名稱：
    BP-1-102
    目錄號：
    HY-100493
    需求量：