EHOP-016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE
- CAS号:1380432-32-5
- 英文名:N4-(9-Ethyl-9H-carbazol-3-yl)-N2-(3-Morpholin-4-yl-propyl)-pyriMidine-2,4-diaMine
- 中文名:EHOP-016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE
- CBNumber:CB82631369
- 分子式:C25H30N6O
- 分子量:430.55
- MOL File:1380432-32-5.mol
- 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
- WGK Germany :3
EHOP-016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE性质、用途与生产工艺
- 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。
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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.
- 更新日期：2024/11/08
- 产品编号：HY-12810
- 产品名称：EHop-016
- CAS编号：
- 包装：5 mg
- 价格：420元
- 更新日期：2024/11/08
- 产品编号：HY-12810
- 产品名称：EHOP-016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE EHop-016
- CAS编号：1380432-32-5
- 包装：10mM * 1mLin DMSO
- 价格：462元
- 公司名称：Novachemistry
- 联系电话：44-20819178-90 02081917890
- 电子邮件：info@novachemistry.com
- 国家：英国
- 产品数：4381
- 优势度：58
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5726
- 优势度：77
