1380432-32-5

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

英文名称 N4-(9-Ethyl-9H-carbazol-3-yl)-N2-(3-Morpholin-4-yl-propyl)-pyriMidine-2,4-diaMine

CAS 1380432-32-5

分子式 C25H30N6O

分子量 430.55

MOL 文件 1380432-32-5.mol

更新日期 2024/05/21 15:12:58

1380432-32-5 结构式

基本信息物理化学性质安全数据图谱信息 EHOP-016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE价格(试剂级) 常见问题列表

基本信息

中文别名

RAC GTPASE抑制剂(EHOP-016)
N4-(9-乙基-9H-咔唑-3-基)-N2-[3-(4-吗啉基)丙基]-2,4-嘧啶二胺

英文别名

EHop-016
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

所属类别

生物化工：Rho 抑制剂

物理化学性质

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

安全数据

WGK Germany3

图谱信息

EHOP-016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE(1380432-32-5)核磁图(¹HNMR)

常见问题列表

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.