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  2. MAPK/ERK Pathway Stem Cell/Wnt
  3. ERK
  4. SCH772984

SCH772984 是一種高選擇性和 ATP 競(jìng)爭(zhēng)性 ERK 抑制劑，對(duì) ERK1 和 ERK2 的 IC50 分別為 4 和 1 nM。SCH772984 在對(duì)天然 MAPK 抑制和耐藥 MAPK 抑制的細(xì)胞中的 BRAF 或 RAS 突變，具有抗腫瘤活性。

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SCH772984 Chemical Structure

SCH772984 Chemical Structure

CAS No. : 942183-80-4

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥2044
In-stock
1 mg ￥719
In-stock
2 mg ￥1050
In-stock
5 mg ￥1438
In-stock
10 mg ￥2046
In-stock
25 mg ￥3376
In-stock
50 mg ￥4726
In-stock
100 mg 現(xiàn)貨 詢(xún)價(jià)
200 mg   詢(xún)價(jià)  
500 mg   詢(xún)價(jià)  

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 135 篇科研文獻(xiàn)

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IF

    SCH772984 purchased from MCE. Usage Cited in: Nat Commun. 2023 Feb 13;14(1):802.  [Abstract]

    SCH772984 upregulates Mbp and Ng2, as well as significantly reduces Cd74 and Erk1/2, in primary neuronal cultures from control and Alzheimer’s disease knock-in mice (Fig. i and j).

    SCH772984 purchased from MCE. Usage Cited in: Acta Biomater. 2019 Feb;85:106-116.  [Abstract]

    Western analysis of related protein expression in the treatment of DBM/CBD-IKVAV-cRGD, DBM/CBD-IKVAV-cRGD + FAK inhibitor PF-573228 or DBM/CBD-IKVAV-cRGD + ERK inhibitor SCH772984.

    SCH772984 purchased from MCE. Usage Cited in: Sci Rep. 2019 Jan 29;9(1):907.  [Abstract]

    HCT116 cells are first treated with different concentrations of PD0325901 or SCH772984 for 36 h and are then treated without or with MG132 for 12 hours before harvested for analysis of the levels of proteins by western blotting using antibodies as indicated.

    SCH772984 purchased from MCE. Usage Cited in: Sci Rep. 2019 Jan 29;9(1):907.  [Abstract]

    KYSE70 cells are first treated with different concentrations of PD0325901 or SCH772984 for 36 hours and are then treated without or with MG132 for 12 hours before cells are harvested for western blotting using antibodies as indicated.

    SCH772984 purchased from MCE. Usage Cited in: Sci Rep. 2019 Jan 29;9(1):907.  [Abstract]

    HCT116 cells are treated with different concentrations of PD0325901 or SCH772984 before cells are harvested for western blotting analysis for ERK1/2 and phosphorylated ERK1/2

    SCH772984 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)+SCH772984 (10 μM) for 30 min, followed by administration of Aβ42 (5 μM) for 6 h.

    SCH772984 purchased from MCE. Usage Cited in: Cancer Res. 2018 Feb 15;78(4):891-908.  [Abstract]

    A549 cells are treated with 10 μM SCH772984 (ERK1/2 inhibitor) or DMSO for 16 hr and analyzed for PSC formation by immunostaining

    SCH772984 purchased from MCE. Usage Cited in: J Immunol Res. 2018 Jun 7;2018:6249085.  [Abstract]

    The level of p-ERK1/2 expression is suppressed by SCH772984. RAW264.7 cells are preincubated with 1 μM SCH772984 for 2h followed by treatment with 20 μg/mL ox-LDL for 24 h.

    SCH772984 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Jan 1;495(1):781-786.  [Abstract]

    Representative images of migrated cells. HUVECs are pretreated with PD98059 (10 μM), SCH772984 (500 nM) or mock control for 2 h, and seeded in upper chambers of transwell inserts. VEGF (100 ng/ml), Scg3 (1 μg/ml) or PBS in medium with reduced FBS is added to bottom chambers in the presence or absence of the inhibitor. After culturing for 4 or 20 h, cells migrated to the lower surface of transwell membrane are stained with DAPI.

    SCH772984 purchased from MCE. Usage Cited in: J Neuroinflammation. 2017 Nov 25;14(1):228.  [Abstract]

    HSP70 release is reversed by ERK1/2 inhibitor in SH-SY5Y cells. SCH772984 (ERK1/2 inhibitor, 2 μM) is given 15 min. Supernatants are collected and analyzed by western blot (n=3).

    SCH772984 purchased from MCE. Usage Cited in: Neurotox Res. 2017 Nov;32(4):535-543.  [Abstract]

    Lithium promotes autophagy flux by activating MEK/ERK pathway in cells. Original Western blot showing LC3-II and p62 abundance following treatment with lithium in the presence of PD184352 and SCH772984 in neurons. Arithmetic means±SEM (n=5) showing LC3-II abundance following treatment with lithium in the presence of PD184352 and SCH772984 in neurons.

    SCH772984 purchased from MCE. Usage Cited in: Faculty of Medicine, Dentistry and Health Sciences. University of Melbourne. 2017 Sep.

    Western blot analysis is performed on protein lysates from exponentially growing melanoma cell lines following 24 hours treatment with 0.1% DMSO as a vehicle control or: GSK1120212 (GSK212) 100 nM; GDC0623 100 nM or SCH772984 1 μM.

    SCH772984 purchased from MCE. Usage Cited in: Department of Dental Pharmacology. Okayama University. 2015.

    The role of Semaphorin4D in bone invasion by oral cancer.

    查看 ERK 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-na?ve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations[1].

    IC50 & Target[1]

    ERK2

    1 nM (IC50)

    ERK1

    4 nM (IC50)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A-375 IC50
    0.004 μM
    Compound: SCH772984
    Inhibition of ERK2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-ERK2 level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis
    Inhibition of ERK2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-ERK2 level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis
    		[PMID: 25977981]
    A-375 IC50
    0.02 μM
    Compound: SCH772984
    Inhibition of ERK1/2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-RSK level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis
    Inhibition of ERK1/2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-RSK level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis
    		[PMID: 25977981]
    A-375 IC50
    0.07 μM
    Compound: SCH772984
    Antiproliferative activity against human A375 cells harboring B-RAF V600E mutant after 72 hrs by Cellomics ArrayScanTM VTI imaging analysis
    Antiproliferative activity against human A375 cells harboring B-RAF V600E mutant after 72 hrs by Cellomics ArrayScanTM VTI imaging analysis
    		[PMID: 25977981]
    A375-SM IC50
    39 nM
    Compound: 1; SCH772984
    Antiproliferative activity against human A375SM cells harboring BRAF V600E mutant measured after 96 hrs by Cell Titer-Glo assay
    Antiproliferative activity against human A375SM cells harboring BRAF V600E mutant measured after 96 hrs by Cell Titer-Glo assay
    		[PMID: 27329786]
    COLO 205 IC50
    16 nM
    Compound: 5; SCH772984
    Antiproliferative activity against human COLO205 cells harboring BRAF V600E/D mutant measured after 4 days
    Antiproliferative activity against human COLO205 cells harboring BRAF V600E/D mutant measured after 4 days
    		[PMID: 30034615]
    HeLa IC50
    > 50 μM
    Compound: 3; SCH772984
    Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs
    Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs
    		[PMID: 32078308]
    HL-60 IC50
    1.06 μM
    Compound: 3; SCH772984
    Antiproliferative activity against human HL60 cells assessed as reduction in cell viability measured after 24 hrs
    Antiproliferative activity against human HL60 cells assessed as reduction in cell viability measured after 24 hrs
    		[PMID: 32078308]
    HT-29 IC50
    59 nM
    Compound: 5; SCH772984
    Antiproliferative activity against human HT-29 cells harboring BRAF V600E/D mutant measured after 4 days
    Antiproliferative activity against human HT-29 cells harboring BRAF V600E/D mutant measured after 4 days
    		[PMID: 30034615]
    HT-29 IC50
    96 nM
    Compound: 5; SCH772984
    Induction of apoptosis in human HT-29 cells harboring BRAF/KRAS mutant by caspase activation assay
    Induction of apoptosis in human HT-29 cells harboring BRAF/KRAS mutant by caspase activation assay
    		[PMID: 29748051]
    MKN-74 IC50
    > 50 μM
    Compound: 3; SCH772984
    Antiproliferative activity against human MKN74 cells assessed as reduction in cell viability measured after 24 hrs
    Antiproliferative activity against human MKN74 cells assessed as reduction in cell viability measured after 24 hrs
    		[PMID: 32078308]
    體外研究
    (In Vitro)

    SCH772984（300 nM；24-48 小時(shí)）導(dǎo)致 SCH772984 敏感黑色素瘤細(xì)胞出現(xiàn) G1 停滯[1]。
    SCH772984（3-300 nM；24 小時(shí)）抑制 ERK 和 RSK 磷酸化[1]。
    SCH772984 在約 88% 和 49% 的 BRAF 突變體（n=25）或 RAS 突變體（n=35）腫瘤系中顯示的 EC50 值低于 500 nM[1]。

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

    Cell Cycle Analysis[1]

    Cell Line: LOX cells (SCH772984-sensitive melanoma cells)
    Concentration: 300 nM
    Incubation Time: 24, 48 hours
    Result: Revealed a G1 arrest as well as an increase in the sub-G1 fraction indicative of apoptosis.

    Western Blot Analysis[1]

    Cell Line: LOX BRAFV600E melanoma cells
    Concentration: 3, 10, 30, 100, 300 nM
    Incubation Time: 24 hours
    Result: A dose-dependent inhibition of phosphorylation of the ERK substrate RSK (T359/S363 phospho-RSK), and also inhibited phosphorylation of residues in the activation loop of ERK itself (T202/Y204 and T185/Y187 of ERK1 and ERK2, respectively).
    體內(nèi)研究
    (In Vivo)

    SCH772984（12.5-50 mg/kg；腹腔注射；每天兩次，持續(xù) 14 天）可使腫瘤消退 98%[1]。
    在 KRAS 突變型胰腺 MiaPaCa 模型中也觀察到了劑量依賴(lài)性抗腫瘤活性，每天兩次 50 mg/kg 劑量下腫瘤消退率為 36%。重要的是，腫瘤消退伴隨著腫瘤組織中 ERK 磷酸化的強(qiáng)烈抑制。根據(jù)發(fā)病率、死亡率或體重減輕來(lái)衡量，SCH772984 在此給藥方案下的耐受性良好[1]。

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

    Animal Model: Female nude mice bearing human LOX BRAFV600E tumors[1]
    Dosage: 12.5, 25, 50 mg/kg
    Administration: Intraperitoneal injection; twice daily for 14 days
    Result: Tumor regressions were observed at all doses, such as 17% at 12.5 mg/kg, 84% at 25 mg/kg, and 98% at 50 mg/kg).
    分子量

    587.67

    Formula

    C33H33N9O2
    CAS 號(hào)
    性狀

    固體

    顏色

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

    DMSO 中的溶解度 : 30 mg/mL (51.05 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 1.7016 mL 8.5082 mL 17.0164 mL
    5 mM 0.3403 mL 1.7016 mL 3.4033 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, 1 year; -20°C, 6 months。-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)?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(qǐng)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(qǐng)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(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： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 3 mg/mL (5.10 mM); 澄清溶液

      此方案可獲得 ≥ 3 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 30.0 mg/mL 的澄清 DMSO 儲(chǔ)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(qǐng)依序添加每種溶劑： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.4 mg/mL (4.08 mM); 澄清溶液

    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： 20% SBE-β-CD in Saline adjusted to pH 4-4.5 with 1 N Acetic

      Solubility: 20 mg/mL (34.03 mM); 澄清溶液; 超聲助溶

    • 方案 二

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

      Solubility: 10 mg/mL (17.02 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

    只
    由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)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(guò) 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
    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(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)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(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)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: 98.97%

    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, 1 year; -20°C, 6 months。-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)?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 1.7016 mL 8.5082 mL 17.0164 mL 42.5409 mL
    5 mM 0.3403 mL 1.7016 mL 3.4033 mL 8.5082 mL
    10 mM 0.1702 mL 0.8508 mL 1.7016 mL 4.2541 mL
    15 mM 0.1134 mL 0.5672 mL 1.1344 mL 2.8361 mL
    20 mM 0.0851 mL 0.4254 mL 0.8508 mL 2.1270 mL
    25 mM 0.0681 mL 0.3403 mL 0.6807 mL 1.7016 mL
    30 mM 0.0567 mL 0.2836 mL 0.5672 mL 1.4180 mL
    40 mM 0.0425 mL 0.2127 mL 0.4254 mL 1.0635 mL
    50 mM 0.0340 mL 0.1702 mL 0.3403 mL 0.8508 mL
    Help & FAQs
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    Inquiry Information

    產(chǎn)品名稱(chēng)：
    SCH772984
    目錄號(hào)：
    HY-50846
    需求量：