Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MGCD-265 analog (Glesatinib) 是一种口服生物可利用的多靶点酪氨酸激酶抑制剂,具有抗肿瘤活性,对 c-Met 和 VEGFR2 的 IC50 分别为 29 nM 和 10 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 433 | 现货 | ||
2 mg | ¥ 625 | 现货 | ||
5 mg | ¥ 952 | 现货 | ||
10 mg | ¥ 1,680 | 现货 | ||
25 mg | ¥ 3,290 | 现货 | ||
50 mg | ¥ 4,780 | 现货 | ||
100 mg | ¥ 6,850 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,130 | 现货 |
产品描述 | MGCD-265 analog (Glesatinib) is an orally bioavailable multitargeted tyrosine kinase inhibitor with potential antineoplastic activity with IC50 of 29 nM and 10 nM for c-Met and VEGFR2, respectively. |
靶点活性 | c-Met:29 nM, VEGFR2:10 nM |
体外活性 | MGCD-265 is a multi-target inhibitor of receptor tyrosine kinases. MGCD-265 potently inhibits Met, MetY1235D, MetM1250T, VEGFR1, VEGF2, VEGF3, Ron, and Tie2, with IC50 values ranging from 1 nM to 7 nM. [1] MGCD-265 inhibits cell proliferation both in c-Met-driven tumor cells (MKN45, MNNG-HOS, and SNU-5) and in non-c-Met-driven tumor cells (HCT116 and MDA-MB-231), with IC50 values of 6 nM–30 nM and 1 μM–3 μM, respectively. In serum starved MKN45 cells, MGCD-265 (40 nM–5 μM) effectively inhibits c-Met phosphorylation and its downstream signaling pathways, including Erk, Akt, Stat3, and Fak. MGCD-265 (6 nM–1 μM) also induces apoptosis in MKN45 cells. |
体内活性 | In c-Met-driven or non-c-Met-driven mice xenograft models of MKN45, U87 mg, MDA-MB-231, COLO205, and A549 tumor cells, MGCD-265 (20 mg/kg–60 mg/kg) inhibits tumor growth and c-Met signaling. MGCD-265 (40 mg/kg) also downregulates genes involved in angiogenesis, including VEGF and IL-8, both in tumor and plasma of mice with U87 mg xenograft. MGCD-265 also inhibits the plasma level of shed-Met. |
激酶实验 | Time-resolved fluorescence resonance energy transfer assay: The c-Met–catalyzed phosphorylation of N-biotinylated peptide (EQEDEPEGDYFEWLE-CONH2) is measured using a time-resolved fluorescence resonance energy transfer assay. [2] The MK-2461 IC50 for Ron, Mer, Flt1, Flt3, Flt4, KDR, PDGFRβ, FGFR1, FGFR2, FGFR3, TrkA, and TrkB are determined using time-resolved fluorescence resonance energy transfer assays similar to the c-Met kinase assay. |
细胞实验 | Cells are treated with MGCD-265 for 72 hours and cell number is determined as a function of mitochondrial activity, following incubation with MTT for 4 hours.(Only for Reference) |
别名 | MGCD-265, Glesatinib |
分子量 | 517.6 |
分子式 | C26H20FN5O2S2 |
CAS No. | 875337-44-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 96 mg/mL (185.5 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.932 mL | 9.66 mL | 19.3199 mL | 48.2998 mL |
5 mM | 0.3864 mL | 1.932 mL | 3.864 mL | 9.66 mL | |
10 mM | 0.1932 mL | 0.966 mL | 1.932 mL | 4.83 mL | |
20 mM | 0.0966 mL | 0.483 mL | 0.966 mL | 2.415 mL | |
50 mM | 0.0386 mL | 0.1932 mL | 0.3864 mL | 0.966 mL | |
100 mM | 0.0193 mL | 0.0966 mL | 0.1932 mL | 0.483 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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