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  2. Protein Tyrosine Kinase/RTK
  3. c-Met/HGFR
  4. SGX-523

SGX523 是一種選擇性和 ATP 競爭性的 MET 抑制劑。 SGX523 有效抑制 MET， IC50 為 4 nM ，比作用于其它他蛋白激酶的選擇性高于 1,000 倍。具有抗腫瘤特性。

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SGX-523 Chemical Structure

SGX-523 Chemical Structure

CAS No. : 1022150-57-7

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥791
In-stock
1 mg ￥361
In-stock
5 mg ￥1000
In-stock
10 mg ￥1500
In-stock
25 mg ￥2950
In-stock
50 mg ￥4700
In-stock
100 mg 現(xiàn)貨 詢價
200 mg   詢價  
500 mg   詢價  

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Customer Review

    SGX-523 purchased from MCE. Usage Cited in: Cancer Res. 2015 Nov 1;75(21):4548-59.  [Abstract]

    c-Myc downregulation is essential for c-Met inhibition caused by growth arrest in MET-addicted cells. EBC-1, NCI-H1993, SNU-5, MKN-45, and HCC827 cells are treated with SGX-523 at 1 μM for 24 or 48 hours followed by immunoblotting analysis of cell-cycle regulators.

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    SGX523 is a exquisitely selective and ATP-competitive MET inhibitor. SGX523 potently inhibits MET with an IC50 of 4 nM and is >1,000-fold selective versus other protein kinases. Antitumor activity[1].

    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    > 10000 nM
    Compound: 1; SGX-523
    Cytotoxicity against human A549 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
    Cytotoxicity against human A549 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
    		[PMID: 27288183]
    HCCLM3 IC50
    24 nM
    Compound: 1; SGX-523
    Cytotoxicity against human HCCLM3 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
    Cytotoxicity against human HCCLM3 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
    		[PMID: 27288183]
    Huh-7 IC50
    > 10000 nM
    Compound: 1; SGX-523
    Cytotoxicity against human HuH7 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
    Cytotoxicity against human HuH7 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
    		[PMID: 27288183]
    MHCC97H IC50
    11 nM
    Compound: 1; SGX-523
    Cytotoxicity against human MHCC97H cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
    Cytotoxicity against human MHCC97H cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
    		[PMID: 27288183]
    MKN-45 IC50
    15 nM
    Compound: 1; SGX-523
    Cytotoxicity against human MKN45 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
    Cytotoxicity against human MKN45 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
    		[PMID: 27288183]
    NCI-H1975 IC50
    > 10000 nM
    Compound: 1; SGX-523
    Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
    Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
    		[PMID: 27288183]
    NCI-H1993 IC50
    25 nM
    Compound: 1; SGX-523
    Cytotoxicity against human NCI-H1993 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
    Cytotoxicity against human NCI-H1993 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
    		[PMID: 27288183]
    NCI-N87 IC50
    > 10000 nM
    Compound: 1; SGX-523
    Cytotoxicity against human NCI-N87 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
    Cytotoxicity against human NCI-N87 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
    		[PMID: 27288183]
    SNU-5 IC50
    3.9 nM
    Compound: 1; SGX-523
    Cytotoxicity against human SNU5 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
    Cytotoxicity against human SNU5 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay
    		[PMID: 27288183]
    體外研究
    (In Vitro)

    SGX523 顯示 ATP 競爭性抑制作用，對活性較低的未磷酸化形式的 MET[MET-KD (0P)，Ki=2.7 nM]與活性較高的磷酸酶[MET- KD (3P)，Ki=23 nM][1]。
    SGX523抑制胃癌和肺癌細胞株的生長，擴增MET 基因，但即使在高微摩爾濃度下，對具有正常 MET 基因拷貝數(shù)的細胞系也沒有影響。對 NSCLC H1993、胃癌 MKN45 和胃癌 Hs746T 細胞的 IC50 分別為 0.02、0.113 和 0.035 μM[1]。
    在 GTL16 細胞 中，抑制 MET 自磷酸化的 50 值為 0.040 μM[1]。
    SGX523 (0.5、1.5、4.6、13.7、41、123、370、1100、3300、10000 nM；1 小時) 抑制 MET 自磷酸化，而不影響 HGF 刺激的 A549 中的總 MET 或細胞外信號調(diào)節(jié)激酶蛋白水平細胞[1]。

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

    Cell Viability Assay[1]

    Cell Line: Gastric cancer cell line GTL16
    Concentration: 4.6, 14, 40, 120, 370, 1100, 3300, 10000 nM
    Incubation Time: 1 hours
    Result: Abolished constitutive signaling induced by MET gene amplification.
    體內(nèi)研究
    (In Vivo)

    SGX523 在體內(nèi)表現(xiàn)出抗腫瘤活性。SGX523 抑制 MET 依賴性腫瘤生長[2]。

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

    Animal Model: Female Harlan nude mice (athymic nu/nu) were s.c. implanted with U87 cells[2]
    Dosage: 10 or 30 mg/kg
    Administration: Oral gavage; twice daily starting at day 5 for 22 days
    Result: Potently inhibited U87MG tumor growth at a dose of 10 mg/kg administered twice daily.
    Led to clear regression of U87MG tumors at 30 mg/kg dosed twice daily.
    Clinical Trial
    分子量

    359.41

    Formula

    C18H13N7S
    CAS 號
    性狀

    固體

    顏色

    Light yellow to 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 : 30 mg/mL (83.47 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)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.7823 mL 13.9117 mL 27.8234 mL
    5 mM 0.5565 mL 2.7823 mL 5.5647 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(nèi)使用， -20°C儲存時，請在1年內(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

    動物實驗：

    以下溶解方案源自文獻，僅供參考，建議您先取少量樣品進行嘗試。

    • 方案 一

      SGX-523 is prepared in 0.5% sodium carboxymethyl cellulose[2].

    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
    計算結(jié)果
    工作液所需濃度 : mg/mL
    純度 & 產(chǎn)品資料

    純度: ≥99.0%

    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(nèi)使用， -20°C儲存時，請在1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 2.7823 mL 13.9117 mL 27.8234 mL 69.5584 mL
    5 mM 0.5565 mL 2.7823 mL 5.5647 mL 13.9117 mL
    10 mM 0.2782 mL 1.3912 mL 2.7823 mL 6.9558 mL
    15 mM 0.1855 mL 0.9274 mL 1.8549 mL 4.6372 mL
    20 mM 0.1391 mL 0.6956 mL 1.3912 mL 3.4779 mL
    25 mM 0.1113 mL 0.5565 mL 1.1129 mL 2.7823 mL
    30 mM 0.0927 mL 0.4637 mL 0.9274 mL 2.3186 mL
    40 mM 0.0696 mL 0.3478 mL 0.6956 mL 1.7390 mL
    50 mM 0.0556 mL 0.2782 mL 0.5565 mL 1.3912 mL
    60 mM 0.0464 mL 0.2319 mL 0.4637 mL 1.1593 mL
    80 mM 0.0348 mL 0.1739 mL 0.3478 mL 0.8695 mL
    Help & FAQs
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      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：
    SGX-523
    目錄號：
    HY-12019
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