1380432-32-5
1380432-32-5 結(jié)構(gòu)式
基本信息
N4-(9-乙基-9H-咔唑-3-基)-N2-[3-(4-嗎啉基)丙基]-2,4-嘧啶二胺
EHop-016, >=98%
EHOP 016
EHOP016
EHOP016
EHOP-016
EHOP 016
EHOP016
EHOP-016
EHOP 016.
4-N-(9-ethylcarbazol-3-yl)-2-N-(3-morpholin-4-ylpropyl)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-Morpholin-4-yl-propyl)-pyriMidine-2,4-diaMine
2,4-Pyrimidinediamine, N4-(9-ethyl-9H-carbazol-3-yl)-N2-[3-(4-morpholinyl)propyl]-
N4-(9-Ethyl-9H-carbazol-3-yl)-N2-[3-(4-morpholinyl)propyl]-2,4-pyrimidinediamine Ehop-016
EHOP-016
N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE
物理化學(xué)性質(zhì)
常見問題列表
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. |