EHOP-016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE
中文名称 | EHOP-016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE |
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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);EHOP-016游离态;N4-(9-乙基-9H-咔唑-3-基)-N2-(3-吗啉丙基)嘧啶-2,4-二胺;EHOP-016,RAC抑制剂 |
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 | 细胞周期;小分子抑制剂;小分子抑制剂,天然产物;细胞生物学试剂;Inhibitors |
Mol文件 | 1380432-32-5.mol |
结构式 | ![]() |
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) |
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密度 | 1.27 |
储存条件 | 2-8°C |
溶解度 | DMSO:可溶10mg/mL,澄清 |
酸度系数(pKa) | 7.30±0.10(Predicted) |
形态 | 粉末 |
颜色 | 白色至米色 |
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%. |
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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更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-12810 | EHop-016 | 5 mg | 420元 | |
2024/08/19 | HY-12810 | EHOP-016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE EHop-016 | 1380432-32-5 | 10mM * 1mLin DMSO | 462元 |