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EHOP-016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE

EHOP-016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE 更多供应商
公司名称: 上海波以尔化工有限公司  
联系电话:
产品介绍: 英文名称:EHOP-016
CAS:1380432-32-5
公司名称: 北京百灵威科技有限公司  
联系电话: 400-666-7788 010-82848833
产品介绍: 英文名称:EHop-016
CAS:1380432-32-5
包装信息:100Mg,10Mg,25Mg 备注:化学试剂、精细化学品、医药中间体、材料中间体
公司名称: 武汉永璨生物科技有限公司  
联系电话: 027-65522453
产品介绍: 英文名称:EHop-016
CAS:1380432-32-5
纯度:98% HPLC 包装信息:50.0mg;100.0mg; 200.0mg;500mg;1g;5g; 10g 备注:科研试剂
公司名称: BOC Sciences  
联系电话: 16314854226
产品介绍: 英文名称:EHop-016
CAS:1380432-32-5
纯度:98% 备注:EHop-016 is a novel potent and selective inhibitor of RAC. EHop-016 inhibits Rac activity in the MDA-MB-435 metastatic cancer cells that overexpress Rac and exhibits high endogenous Rac activity. The
公司名称: 上海皓元医药股份有限公司  
联系电话: 86-21-58998985
产品介绍: 英文名称:EHop-016
CAS:1380432-32-5
纯度:>98% 包装信息:700RMB/10mg 备注:试剂级
最新发布供应信息
Rac GTPase抑制剂(EHop-016)_上海泽叶生物科技有限公司
2021/8/3 13:22:00
EHOP-016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE
生物活性体外研究体内研究
中文名称:EHOP-016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE
中文同义词:N4-(9-乙基-9H-咔唑-3-基)-N2-[3-(4-吗啉基)丙基]-2,4-嘧啶二胺;RAC GTPASE抑制剂(EHOP-016)
英文名称:N4-(9-Ethyl-9H-carbazol-3-yl)-N2-(3-Morpholin-4-yl-propyl)-pyriMidine-2,4-diaMine
英文同义词:EHop-016;EHOP-016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE;N4-(9-Ethyl-9H-carbazol-3-yl)-N2-(3-Morpholin-4-yl-propyl)-pyriMidine-2,4-diaMine;N4-(9-Ethyl-9H-carbazol-3-yl)-N2-[3-(4-morpholinyl)propyl]-2,4-pyrimidinediamine;N4-(9-Ethyl-9H-carbazol-3-yl)-N2-[3-(4-morpholinyl)propyl]-2,4-pyrimidinediamine Ehop-016;EHop-016, >=98%;EHOP016; EHOP-016; EHOP 016; EHOP016; EHOP-016; EHOP 016.;EHOP 016;EHOP016
CAS号:1380432-32-5
分子式:C25H30N6O
分子量:430.55
EINECS号:
相关类别:细胞生物学试剂;细胞周期;小分子抑制剂;小分子抑制剂,天然产物;Inhibitors
Mol文件:1380432-32-5.mol
EHOP-016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE
EHOP-016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE 性质
沸点 633.9±65.0 °C(Predicted)
密度 1.27
储存条件 2-8°C
溶解度 DMSO: soluble10mg/mL, clear
酸度系数(pKa)7.30±0.10(Predicted)
形态powder
颜色white to beige
EHOP-016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE 用途与合成方法
生物活性EHop-016 是一种有效的选择性的 Rac GTPase Rac1 和 Rac3 抑制剂。EHop-016 在 MDA-MB-435 细胞中抑制 Rac1 活性,IC50 为 1.1 μM。EHop-016 抑制 Vav2 与 Rac,Rac 激活的 PAK1 相互作用,片状脂蛋白形成和细胞迁移。
体外研究

EHop-016 (1-10 μM; 24 hours; MDA-MB-435 cells) treatment inhibits Rac1 and Rac3 activity. At higher concentrations, EHop-016 inhibits the close homolog Cdc42. In MDA-MB-435 cells that demonstrate high active levels of the Rac GEF Vav2, EHop-016 inhibits the association of Vav2 with a nucleotide-free Rac1(G15A) .
EHop-016 also inhibits the Rac activity of MDA-MB-231 metastatic breast cancer cells and reduces Rac-directed lamellipodia formation in both cell lines. EHop-016 decreases Rac downstream effects of PAK1 (p21-activated kinase 1) activity and directed migration of metastatic cancer cells.
EHop-016 affectes cell viability by down-regulating Akt and Jun kinase activities and c-Myc and Cyclin D expression, as well as increasing caspase 3/7 activities in metastatic cancer cells.

Western Blot Analysis

Cell Line: MDA-MB-435 cells
Concentration: 1 μM, 2 μM, 4 μM, 5 μM, 10 μM
Incubation Time: 24 hours
Result: The activity Rac3 was inhibited by 58%.
体内研究

EHop-016 (10-25 mg/kg; intraperitoneal injection; 3 times a week; for 55 days; nu/nu mice) treatment significantly reduces mammary fat pad tumor growth, metastasis, and angiogenesis.

Animal Model: Female athymic nu/nu mice (4-5 weeks old) injected with GFP-MDA-MB-435 cells
Dosage: 10 mg/kg, 25 mg/kg
Administration: Intraperitoneal injection; 3 times a week; for 55 days
Result: Significantly reduced mammary fat pad tumor growth, metastasis, and angiogenesis.
安全信息
WGK Germany 3
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