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  2. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease
  3. SHP2 Phosphatase
  4. SHP099

SHP099 是一種變構(gòu) SHP2 抑制劑，對 SHP2, SHP2D61Y, SHP2E69K, SHP2A72V, SHP2E76K 的 IC50s 為 0.690, 1.241, 0.416, 1.968, 2.896 μM。SHP099 抑制癌細(xì)胞生長，例如 MV4-11 和 TF-1 細(xì)胞 (IC50: 0.32 和 1.73 μM)。SHP099 抑制 RAS-ERK 信號傳導(dǎo)并抑制腫瘤生長。

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SHP099 Chemical Structure

SHP099 Chemical Structure

CAS No. : 1801747-42-1

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3.  試用裝只面向終端客戶。

規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥620
In-stock
5 mg ￥800
In-stock
10 mg ￥1450
In-stock
50 mg ￥4800
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 SHP099:

MCE 顧客使用本產(chǎn)品發(fā)表的 61 篇科研文獻(xiàn)

WB

    SHP099 purchased from MCE. Usage Cited in: Cancer Discov. 2018 Oct;8(10):1237-1249.  [Abstract]

    Immunoblots of whole cell lysates or GST-RBD-precipitated (RAS-GTP, KRASGTP and NRAS-GTP) lysates from PDAC cells treated with DMSO, SHP099 10 μM, AZD6244 1 μM, or both drugs for the times indicated.

    SHP099 purchased from MCE. Usage Cited in: Nat Commun. 2019 Apr 1;10(1):1473.  [Abstract]

    SHP099 inhibits IRS1-AP2 interaction in primary hepatocytes.

    SHP099 purchased from MCE. Usage Cited in: Hepatology. 2018 Jul;68(1):333-348.  [Abstract]

    Primary human HSCs are treated with SHP099 for 1 hour. PDGF-BB is added and cells are cultured for 12 additional hours. Whole cell lysates and EVs are examined by WB (n=6).

    SHP099 purchased from MCE. Usage Cited in: Open Biol. 2017 May;7(5). pii: 170066.  [Abstract]

    Comparing the effects of SHP2 degradation and allosteric inhibition on Ras/MAPK signalling. (a) Human U2OS, A549, K-562 and MDA-MB-468 cells are treated with DMSO control or 1, 5 and 10 μM SHP099 for 2 h prior to lysis. Extracts (10 μg protein) are resolved by SDS-PAGE and transferred to nitrocellulose membranes, which are subjected to western blotting with the indicated antibodies. (b) Uninfected U2OS cells (WT) or cells infected with retroviruses encoding VHL, aCS3 and VHL-aCS3 are treated wit

    • 生物活性

    • 實(shí)驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    SHP099 is an allosteric SHP2 inhibitor, with IC50s of 0.690, 1.241, 0.416, 1.968, 2.896 μM for SHP2, SHP2D61Y, SHP2E69K, SHP2A72V, SHP2E76K. SHP099 inhibits cancer cell growth, such as MV4-11 and TF-1 cell (IC50: 0.32 and 1.73 μM). SHP099 inhibits RAS-ERK signaling and inhibits tumor growth[1][2].

    IC50 & Target

    IC50: 70 nM (SHP2)[1]
    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    4T1 IC50
    119.3 μM
    Compound: SHP099
    Antiproliferative activity against mouse 4T1 cells assessed as cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse 4T1 cells assessed as cell viability incubated for 72 hrs by CCK-8 assay
    		[PMID: 36097406]
    ASPC1 IC50
    64.04 μM
    Compound: SHP099
    Antiproliferative activity against human ASPC1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human ASPC1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    		[PMID: 36097406]
    BaF3 IC50
    19.86 μM
    Compound: SHP-099
    Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
    Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
    		[PMID: 33582386]
    BXPC-3 IC50
    72.86 μM
    Compound: SHP099
    Antiproliferative activity against human BXPC-3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human BXPC-3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    		[PMID: 36097406]
    Capan-2 IC50
    15.67 μM
    Compound: SHP-099
    Cytotoxicity against human Capan-2 cells harbouring K-ras mutant assessed as reduction in cell viability incubated for 144 hrs
    Cytotoxicity against human Capan-2 cells harbouring K-ras mutant assessed as reduction in cell viability incubated for 144 hrs
    		[PMID: 33582386]
    Detroit 562 IC50
    6.47 μM
    Compound: 2; SHP099
    Antiproliferative activity against human Detroit 562 cells after 24 hrs by Celltiter-Glo assay
    Antiproliferative activity against human Detroit 562 cells after 24 hrs by Celltiter-Glo assay
    		[PMID: 30688459]
    KYSE-520 cell line IC50
    1.4 μM
    Compound: 1
    Antiproliferative activity against human KYSE520 cells assessed as reduction in cell viability measured after 5 days by Celltiter-Glo assay
    Antiproliferative activity against human KYSE520 cells assessed as reduction in cell viability measured after 5 days by Celltiter-Glo assay
    		[PMID: 27347692]
    KYSE-520 cell line IC50
    1.4 μM
    Compound: 2; SHP099
    Antiproliferative activity against human KYSE520 cells added 24 hrs after cell plating and measured on day 5 by Celltiter-Glo assay
    Antiproliferative activity against human KYSE520 cells added 24 hrs after cell plating and measured on day 5 by Celltiter-Glo assay
    		[PMID: 30688459]
    KYSE-520 cell line IC50
    13.22 μM
    Compound: SHP099
    Antiproliferative activity against human KYSE520 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human KYSE520 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    		[PMID: 36097406]
    KYSE-520 cell line IC50
    18.2 μM
    Compound: 1; SHP099
    Growth inhibition of human KYSE520 cells measured after 4 days by WST8 assay
    Growth inhibition of human KYSE520 cells measured after 4 days by WST8 assay
    		[PMID: 32437146]
    MDA-MB-468 IC50
    29.9 μM
    Compound: SHP099
    Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 2 to 4 days by CCK-8 assay
    Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 2 to 4 days by CCK-8 assay
    		[PMID: 31784318]
    MDA-MB-468 IC50
    49.6 μM
    Compound: SHP099
    Antiproliferative activity against human MDA-MB-468 3D spheroids assessed as reduction in cell viability after 2 to 4 days by CCK-8 assay
    Antiproliferative activity against human MDA-MB-468 3D spheroids assessed as reduction in cell viability after 2 to 4 days by CCK-8 assay
    		[PMID: 31784318]
    MOLM-14 IC50
    0.9 μM
    Compound: SHP099
    Antiproliferative activity against human MOLM14 cells after 3 days by CellTiter-Glo luminescence assay
    Antiproliferative activity against human MOLM14 cells after 3 days by CellTiter-Glo luminescence assay
    		[PMID: 29089257]
    MV4-11 IC50
    0.24 μM
    Compound: SHP099
    Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs in presence of SAHA by CCK-8 assay
    Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs in presence of SAHA by CCK-8 assay
    		[PMID: 36097406]
    MV4-11 IC50
    0.475 nM
    Compound: 1; SHP099
    Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
    Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
    		[PMID: 33780898]
    MV4-11 IC50
    0.572 μM
    Compound: 1; SHP099
    Cytotoxicity against human MV4-11 cells assessed as cell viability measured after 72 hrs by MTS assay
    Cytotoxicity against human MV4-11 cells assessed as cell viability measured after 72 hrs by MTS assay
    		[PMID: 33780898]
    MV4-11 IC50
    0.803 μM
    Compound: 1; SHP099
    Cytotoxicity against CRBN knock out human MV4-11 cells assessed as cell viability measured after 72 hrs by MTS assay
    Cytotoxicity against CRBN knock out human MV4-11 cells assessed as cell viability measured after 72 hrs by MTS assay
    		[PMID: 33780898]
    MV4-11 IC50
    1 μM
    Compound: 1; SHP099
    Growth inhibition of human MV4-11 cells measured after 4 days by WST8 assay
    Growth inhibition of human MV4-11 cells measured after 4 days by WST8 assay
    		[PMID: 32437146]
    MV4-11 IC50
    1.75 μM
    Compound: SHP099
    Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    		[PMID: 36097406]
    SW1990 IC50
    104.8 μM
    Compound: SHP099
    Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    		[PMID: 36097406]
    體外研究
    (In Vitro)

    SHP099 與 SHP2 的 X 射線共晶揭示了與堿性胺和 Phe113 主鏈羰基的新相互作用。SHP099 抑制細(xì)胞增殖 (KYSE-520 模型)，IC50 為 1.4 μM。SHP099 在 Caco-2 細(xì)胞中表現(xiàn)出高溶解性和高滲透性且無明顯外排[1]。
    SHP099 同時結(jié)合 N 端 SH2、C 端 SH2 和蛋白酪氨酸磷酸酶結(jié)構(gòu)域的界面，從而通過變構(gòu)機(jī)制抑制 SHP2 活性。SHP099 通過抑制 RAS–ERK 信號通路抑制受體酪氨酸激酶驅(qū)動的人類癌細(xì)胞的增殖[2]。

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

    在單劑量 30 和 100 mg/kg (分別為紅線和藍(lán)線) 后，在異種移植物中觀察到藥效學(xué)標(biāo)記物 p-ERK 的劑量依賴性暴露和調(diào)節(jié)。每日口服劑量 10 或 30 mg/kg 分別產(chǎn)生 19% 和 61% 的腫瘤生長抑制。達(dá)到 100 mg/kg 時腫瘤停滯[1]。

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

    352.26

    Formula

    C16H19Cl2N5
    CAS 號
    性狀

    固體

    顏色

    Light yellow to yellow

    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 6 months
    -20°C 1 month
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗： 

    DMSO 中的溶解度 : 12 mg/mL (34.07 mM; 超聲助溶; 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)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.8388 mL 14.1941 mL 28.3881 mL
    5 mM 0.5678 mL 2.8388 mL 5.6776 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, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(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(shí)驗：

    請根據(jù)您的 實(shí)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(shí)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(shí)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: ≥ 1.2 mg/mL (3.41 mM); 澄清溶液

      此方案可獲得 ≥ 1.2 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 12.0 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: ≥ 1.2 mg/mL (3.41 mM); 澄清溶液

      此方案可獲得 ≥ 1.2 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 12.0 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： 0.5% CMC-Na/saline water

      Solubility: 10 mg/mL (28.39 mM); 懸濁液; 超聲助溶

    動物溶解方案計算器
    請輸入動物實(shí)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(shí)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(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: 99.80%

    參考文獻(xiàn)
    Kinase Assay
    [1]

    The inhibition of SHP2 from the tested compounds (SHP099) concentrations varying from 0.003-100 μM is monitored using an assay in which 0.5 nM of SHP2 is incubated with of 0.5 μM of peptide IRS1_pY1172(dPEG8)pY1222. After 30-60 minutes incubation at the surrogate substrate, DiFMUP is added to the reaction and incubated at 25 °C for 30 minutes. The reaction is then quenched by the addition of 5 μL of a 160 μM solution of bpV(Phen). The fluorescence signal is monitored using a microplate reader using excitation and emission wavelengths of 340 nm and 450 nm, respectively[1].

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

    Cells are plated onto 96-well plates in 100 μL medium. SHP099 with various concentrations (1.25, 2.5, 5, 10, 20 μM) are added 24 h after cell plating. At day 5, 50 μL Celltiter-Glo reagent is added, and the luminescent signal is determined[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, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(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 2.8388 mL 14.1941 mL 28.3881 mL 70.9703 mL
    5 mM 0.5678 mL 2.8388 mL 5.6776 mL 14.1941 mL
    10 mM 0.2839 mL 1.4194 mL 2.8388 mL 7.0970 mL
    15 mM 0.1893 mL 0.9463 mL 1.8925 mL 4.7314 mL
    20 mM 0.1419 mL 0.7097 mL 1.4194 mL 3.5485 mL
    25 mM 0.1136 mL 0.5678 mL 1.1355 mL 2.8388 mL
    30 mM 0.0946 mL 0.4731 mL 0.9463 mL 2.3657 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：
    SHP099
    目錄號：
    HY-100388
    需求量：