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
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：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;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE 用途与合成方法
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. |
EHOP-016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-11-08 | HY-12810 | 5 mg | 420 | ||
| 2024-11-08 | HY-12810 | EHOP-016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE | 1380432-32-5 | 10mM * 1mLin DMSO | 462 |
