化合物 ENMD-2076|T2358|TargetMol

ENMD-2076
934353-76-1

￥347 1mg 起订

￥468 2mg 起订

￥689 5mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 ENMD-2076

英文名称：: ENMD-2076

CAS号：: 934353-76-1

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: ≥95%

产品类别：: 抑制剂

货号：: T2358

Product Introduction

Bioactivity

名称	ENMD-2076
描述	ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα.
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)
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.
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
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 97 mg/mL (258.3 mM) H2O : 1 mg/mL (2.66 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble)
关键字	Cluster of differentiation antigen 135 \| FLT3 \| Aurora Kinase \| Inhibitor \| Apoptosis \| Fibroblast growth factor receptor \| CD135 \| VEGFR \| Platelet-derived growth factor receptor \| ENMD 2076 \| ENMD2076 \| FGFR \| ENMD-2076 \| Vascular endothelial growth factor receptor \| Fms like tyrosine kinase 3 \| PDGFR \| Src \| inhibit
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ENMD-2076|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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