| 中文名称: | SU11274 | ||||
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| 英文名称: | SU11274 | ||||
| 别名: | SU11274 抑制剂;N-(3-氯苯基)-N-甲基-3-[[3,5-二甲基-4-[(4-甲基哌嗪-1-基)羰基-1H-吡咯-2-基]亚甲基]-2-氧代-2,3-二氢-1H-吲哚-5-磺酰胺 PKI-SU11274 | ||||
| CAS No: | 658084-23-2 | 分子式: | C28H30ClN5O4S | 分子量: | 568.09 |
| CAS No: | 658084-23-2 | ||||
| 分子式: | C28H30ClN5O4S | ||||
| 分子量: | 568.09 | ||||
基本信息
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产品编号：S10690 |
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产品名称：SU11274 |
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CAS: |
658084-23-2 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
568.09 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
92mg/mL (161.94mM) |
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Ethanol |
2mg/mL (3.52mM) |
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Water |
Insoluble |
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体内（现配现用） |
30% PEG400+0.5% Tween80+5% propylene glycol |
30mg/mL |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
1.7603mL |
8.8014mL |
17.6028mL |
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5mM |
0.3521mL |
1.7603mL |
3.5206mL |
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10mM |
0.1760mL |
0.8801mL |
1.7603mL |
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50mM |
0.0352mL |
0.1760mL |
0.3521mL |
生物活性
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产品描述 |
一种选择性的 Met 抑制剂，IC50 值为 10nM，对 PGDFRβ，EGFR 或 Tie2 没有抑制作用。 |
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靶点/IC50 |
IC50: 10nM (Met) |
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体外研究 |
SU11274 exhibits greater than 50-fold selectivity for Met versus Flk and more than 500 times selectivity versus other tyrosine kinases such as FGFR-1, c-src, PDGFbR, and EGFR. SU11274 inhibits the phosphorylation of key regulators of the PI3K pathway,including AKT, FKHR, or GSK3β. SU11274 treatment inhibits the growth of TPR-MET-transformed BaF3 cells in a dose-dependent manner with IC50 of < 3 μM in the absence of interleukin 3, without growth inhibition of BaF3 cells.transformed by other oncogenic tyrosine kinases, including BCR-ABL, TEL-JAK2, TEL-ABL, andTEL-PDGFβR. In addition to cell growth, SU11274 treatment significantly inhibits the migration of BaF3. TPR-MET cells by 44.8% and 80% at 1μM and 5μM, respectively.SU11274 inhibits HGF-dependent phosphorylation of Met as well as HGF-dependent cell proliferation and motility with an IC50 of 1-1.5μM. In H69 and H345 cells which have functional Met receptor, SU11274 inhibits the HGFinduced cell growth with IC50 of 3.4μMand6.5μM,respectively.SU11274 induces G1 cell cycle arrest with cells in G1 phase increased from 42.4% to 70.6% at 5μM, and induces caspase-dependent apoptosis by 24% at 1μM. SU11274 inhibits cell viability in c-Met-expressing non-small cell lung cancer (NSCLC) cells with IC50 values of 0.8-4.4μM,andabrogates hepatocyte growth factor-induced phosphorylation of c-Met and its downstream signaling. |
推荐实验方法(仅供参考)
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激酶实验： |
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A chimeric protein is constructed containing the cytoplasmic domain of human c-Met fused to Glutathione S-transferase(GST) and expressed in SF9 cells. The c-Met kinase GST-fusion protein is used for an ELISA-based Met biochemical assay using the random copolymer poly(Glu:Tyr) (4:1) immobilized on microtiter plates as a substrate. IC50 value is determined with variouscon centrations of SU11274 in a buffer containing 5μM ATP and 10 mM MnCl2, 50mM HEPES (pH 7.5), 25mM NaCl, 0.01% BSA, and 0.1 mM Na orthovanadate. The kinase reaction is performed for 5 minutes at room temperature. The extent of substrate phosphorylation is measured using horseradis peroxidase-conjugated anti-pTyr antibodies. |
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细胞实验: |
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Cells are exposed to various concentrations of SU11274 in the presence or absence of HGF for 24, 48, and 72 hours. The number of viable cells is determined using the MTT assay or trypan blue exclusion. Cell Cycle and apoptosis are measured by fluorescence-activated cell sorter analysis via propidium iodide staining and Annexin V-positive staining, respectively. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
