Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ENMD2076是一种多靶点激酶抑制剂,抑制Aurora A、Flt3、KDR/VEGFR2、Flt4/VEGFR3、FGFR1、FGFR2、Src、PDGFRα的IC50值分别为1.86、14、58.2、15.9、92.7、70.8、20.2 and 56.4 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 347 | 现货 | ||
2 mg | ¥ 468 | 现货 | ||
5 mg | ¥ 689 | 现货 | ||
10 mg | ¥ 1,160 | 现货 | ||
25 mg | ¥ 2,080 | 现货 | ||
50 mg | ¥ 3,290 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 773 | 现货 |
产品描述 | ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα. |
靶点活性 | FLT3:1.86 nM, Aurora A:14 nM, RET:10.4 nM, Src:20.2 nM, VEGFR3/FLT4:15.9 nM |
体外活性 | 在MDA-MB-231异种移植模型中, ENMD-2076可以抑制形成新血管,同时使形成的血管发生退化.在HT29异种移植模型中,ENMD-2076对Flt3以及VEGFR2 / KDR和FGFR1 / 2的激活持续发挥抑制作用.在H929人浆细胞瘤异种移植物中,口服ENMD-2076(50-200 mg / kg /day),其中磷酸 - 组蛋白3(pH3),Ki-67显著降低,裂解的胱天蛋白酶-3显著增加. |
体内活性 | ENMD-2076作用于PI3K/AKT通路,下调凋亡抑制蛋白。ENMD-2076能够抑制aurora A和B激酶,且诱导细胞周期停在G2/M 期。在多种作用于血管生成的激酶中(IC50=1.86-120 nM),ENMD-2076能够发挥作用,比如VEGFR2/KDR 和VEGFR3, FGFR1和FGFR2, 及PDGFRα。在多种人类实体瘤和血癌细胞系中(IC50=0.025 -0.7 μM),ENMD-2076使细胞停滞在G2/M 期,诱导细胞凋亡 |
激酶实验 | Kinase assays: Recombinant Aurora A and B kinase enzymes and appropriate PanVera Z'-Lyte kinase assay kits are purchased. Assays are carried out in kinase assay buffer (50 mM of HEPES, pH 7.5, 10 mM of MgCl2, 5 mM of EGTA, 0.05% Brij-35) supplemented with 2 mM of DTT. Activities are determined at an ATP concentration equivalent to the apparent Km for each enzyme, and an enzyme concentration that results in approximately 30% phosphorylation of the peptide substrate after 1 hour. Dose–response curves of relative enzyme activity versus ENMD-2076 concentration are plotted with Grafit and used to calculate IC50 values. Potency of ENMD-2076 free base against a select panel of 100 kinase enzymes is determined using the SelectScreen kinase profiling service. ATP concentrations are at the apparent Km for each enzyme or 100 μM if the apparent Km could not be reached. Percent inhibition is determined at an ENMD-2076 free base concentration of 1 μM; for kinases where significant inhibition is noted, IC50 values are determined by generating full 10-point dose–response curves. |
细胞实验 | The antiproliferative effect of ENMD-2076 on adherent tumor cell lines is measured by plating 500 cells per well in a 96-well plate and incubating with ENMD-2076 for 96 hours. Cellular proliferation is measured using the sulforhodamine B assay. The leukemia-derived, nonadherent cell lines are assayed by plating 5 × 103 cells per well in a 96-well plate. The cells are incubated with ENMD-2076 for 48 hours and then survival is assayed using the Alamar Blue reagent. To measure the effect of ENMD-2076 on VEGF- and fibroblast growth factor (FGF)-induced proliferation of human umbilical vein endothelial cell (HUVEC), cells are serum starved for 6 hours, then treated with ENMD-2076 free base, and stimulated with 5 ng/mL bFGF or 25 ng/mL VEGF (R and D Systems) for 72 hours. Cell proliferation is measured using WST-(Only for Reference) |
分子量 | 375.47 |
分子式 | C21H25N7 |
CAS No. | 934353-76-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 97 mg/mL (258.3 mM)
H2O: 1 mg/mL (2.66 mM)
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 / H2O | 1 mM | 2.6633 mL | 13.3166 mL | 26.6333 mL | 66.5832 mL |
DMSO | 5 mM | 0.5327 mL | 2.6633 mL | 5.3267 mL | 13.3166 mL |
10 mM | 0.2663 mL | 1.3317 mL | 2.6633 mL | 6.6583 mL | |
20 mM | 0.1332 mL | 0.6658 mL | 1.3317 mL | 3.3292 mL | |
50 mM | 0.0533 mL | 0.2663 mL | 0.5327 mL | 1.3317 mL | |
100 mM | 0.0266 mL | 0.1332 mL | 0.2663 mL | 0.6658 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。
ENMD-2076 934353-76-1 Angiogenesis Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic Tyrosine Kinase/Adaptors Aurora Kinase Src PDGFR c-RET FLT VEGFR FGFR Cluster of differentiation antigen 135 FLT3 Inhibitor Fibroblast growth factor receptor CD135 Platelet-derived growth factor receptor ENMD 2076 ENMD2076 Vascular endothelial growth factor receptor Fms like tyrosine kinase 3 inhibit inhibitor