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

SGX523 是一种选择性和 ATP 竞争性的 MET 抑制剂。 SGX523 有效抑制 MET， IC50 为 4 nM ，比作用于其它他蛋白激酶的选择性高于 1,000 倍。具有抗肿瘤特性。

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SGX-523 Chemical Structure

SGX-523 Chemical Structure

CAS No. : 1022150-57-7

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1 mg ￥361
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5 mg ￥1000
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10 mg ￥1500
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25 mg ￥2950
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50 mg ￥4700
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Customer Review

SGX-523 相关抗体

Top Publications Citing Use of Products

    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

    • 纯度 & 产品资料

    • 参考文献

    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].

    细胞效力
    (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]
    体外研究
    (In Vitro)

    SGX523 显示 ATP 竞争性抑制作用，对活性较低的未磷酸化形式的 MET[MET-KD (0P)，Ki=2.7 nM]与活性较高的磷酸酶[MET- KD (3P)，Ki=23 nM][1]。
    SGX523抑制胃癌和肺癌细胞株的生长，扩增MET 基因，但即使在高微摩尔浓度下，对具有正常 MET 基因拷贝数的细胞系也没有影响。对 NSCLC H1993、胃癌 MKN45 和胃癌 Hs746T 细胞的 IC50 分别为 0.02、0.113 和 0.035 μM[1]。
    在 GTL16 细胞 中，抑制 MET 自磷酸化的 50 值为 0.040 μM[1]。
    SGX523 (0.5、1.5、4.6、13.7、41、123、370、1100、3300、10000 nM；1 小时) 抑制 MET 自磷酸化，而不影响 HGF 刺激的 A549 中的总 MET 或细胞外信号调节激酶蛋白水平细胞[1]。

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

    SGX-523 相关抗体:

    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.
    体内研究
    (In Vivo)

    SGX523 在体内表现出抗肿瘤活性。SGX523 抑制 MET 依赖性肿瘤生长[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 号
    性状

    固体

    颜色

    Light yellow to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 30 mg/mL (83.47 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    以下溶解方案源自文献，仅供参考，建议您先取少量样品进行尝试。

    • 方案 一

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

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料

    纯度: ≥99.0%

    COA (289 KB) HNMR (86 KB)

    产品使用指南 (1538 KB)
    参考文献

    SGX-523 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 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
    • 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.

    Keywords:

    SGX-5231022150-57-7SGX523SGX 523c-Met/HGFRexquisitelyselectiveMETantitumorInhibitorinhibitorinhibit

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    目录号：
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