中文名称:

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

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)

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:

细胞生物学试剂;细胞周期;小分子抑制剂;小分子抑制剂，天然产物;Inhibitors

Mol文件:

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

形态

powder

酸度系数(pKa)

7.30±0.10(Predicted)

颜色

white to beige

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%.

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.

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.

WGK Germany 

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