Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MK-2461 是 ATP 竞争性的 c-Met 抑制剂, 平均 IC50 值为 2.5 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 497 | 现货 | ||
2 mg | ¥ 747 | 现货 | ||
5 mg | ¥ 1,490 | 现货 | ||
10 mg | ¥ 2,660 | 现货 | ||
25 mg | ¥ 4,480 | 现货 | ||
50 mg | ¥ 6,390 | 现货 | ||
100 mg | ¥ 8,750 | 现货 | ||
500 mg | ¥ 17,500 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,620 | 现货 |
产品描述 | MK-2461 is a novel inhibitor that targets multiple proteins and competitively binds to ATP sites, specifically inhibiting the activated c-Met protein with an average inhibitory concentration (IC50) of 2.5 nM. |
靶点活性 | c-Met:2.5 nM |
体外活性 | MK-2461 also potently inhibits FGFR1, FGFR2, FGFR3, KDR, TrkA, TrkB, and Flt4 with IC50 of 65 nM, 39 nM, 50 nM, 44 nM, 46 nM, 61 nM, and 78 nM, respectively. Compared with wild-type c-Met, MK-2461 more potently inhibits the activity of oncogenic c-Met kinase mutants such as N1100Y, Y1230C, Y1230H, Y1235D, and M1250T with IC50 of 1.5 nM, 1.5 nM, 1.0 nM, 0.5 nM, and 0.4 nM, respectively. MK-2461 binds more strongly to phosphorylated c-Met than to unphosphorylated c-Met. MK-2461 potently inhibits ATP-induced autophosphorylation of the COOH-terminal docking domain of c-Met, but not the activation loop. In contrast, MK-2461 inhibits phosphorylation of the activation loop of FGFR2 (Y653/Y654) in Kato III cells and PDGFRα (Y849) in H1703 cells with IC50 of <0.3 μM. MK-2461 inhibits HGF-induced mitogenesis of 4MBr-5 cells with IC50 of 204 nM, and HGF-induced migration of HPAF II cells with IC50 of 404 nM, as well as HGF-induced branching tubulogenesis of MDCK cells. In addition, MK-2461 potently inhibits IL-3-independent proliferation of 32D cells transformed with Tpr-Met or Tpr-Met (Y362C) mutant with IC50 of ~100 nM. MK-2461 significantly inhibits the proliferation of a large panel of tumor cell lines, especially potent against tumor cells harbored genomic amplification of MET or FGFR2. [1] |
体内活性 | MK-2461 treatment significantly inhibits c-Met (Y1349) phosphorylation in GTL-16 tumors with IC50 of ~1 μM. Oral administration of MK-2461 at 10 mg/kg, 50 mg/kg, and 100 mg/kg twice daily as well as 200 mg/kg once daily effectively suppresses tumor growth of GTL-16 xenografts in mice by 62%, 77%, 75%, and 90%, respectively. Similarly, MK-2461 treatment at 134 mg/kg twice daily inhibits the growth of NIH3T3 tumors harboring c-Met single nucleotide mutants T3936C and T3997C, by 78% and 62%, respectively. [1] |
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 exposed to various concentrations of MK-2461 for 72 hours. The viability of tumor cells is measured using the ViaLight PLUS kit.(Only for Reference) |
别名 | MK2461 |
分子量 | 495.55 |
分子式 | C24H25N5O5S |
CAS No. | 917879-39-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 92 mg/mL (185.7 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.018 mL | 10.0898 mL | 20.1796 mL | 50.449 mL |
5 mM | 0.4036 mL | 2.018 mL | 4.0359 mL | 10.0898 mL | |
10 mM | 0.2018 mL | 1.009 mL | 2.018 mL | 5.0449 mL | |
20 mM | 0.1009 mL | 0.5045 mL | 1.009 mL | 2.5224 mL | |
50 mM | 0.0404 mL | 0.2018 mL | 0.4036 mL | 1.009 mL | |
100 mM | 0.0202 mL | 0.1009 mL | 0.2018 mL | 0.5045 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。
MK-2461 917879-39-1 Tyrosine Kinase/Adaptors c-Met/HGFR MK2461 inhibit Inhibitor MK 2461 inhibitor