2-Methyl-2-(3-methyl-4-((4-(methylamino)-5-(trifluoromethyl)-pyrimidin-2-yl)amino)-1H-pyrazol-
GNE-0877
CAS: 1374828-69-9
Molecular Formula: C14H16F3N7
2-Methyl-2-(3-methyl-4-((4-(methylamino)-5-(trifluoromethyl)-pyrimidin-2-yl)amino)-1H-pyrazol- - Names and Identifiers
2-Methyl-2-(3-methyl-4-((4-(methylamino)-5-(trifluoromethyl)-pyrimidin-2-yl)amino)-1H-pyrazol- - Physico-chemical Properties
| Molecular Formula | C14H16F3N7 |
| Molar Mass | 339.32 |
| Density | 1.36±0.1 g/cm3(Predicted) |
| Melting Point | 121 - 122°C |
| Boling Point | 506.3±60.0 °C(Predicted) |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | White to Off-White |
| pKa | 3.87±0.10(Predicted) |
| Storage Condition | -20°C, Inert atmosphere |
| In vitro study | GNE-0877 significantly inhibited LRRK2 cell activity with an IC50 of 3 nM and showed low conversion in human liver microsomes and hepatocytes. In addition, GNE-0877 was also a reversible CYP1A2 inhibitor with an IC50 of 0.7 μm. GNE-0877 significantly inhibited LRRK2 cell activity with an IC50 of 3 nM and showed low conversion in human liver microsomes and hepatocytes. In addition, GNE-0877 was also a reversible CYP1A2 inhibitor with an IC50 of 0.7 μm. |
| In vivo study | In vivo, GNE-0877 showed good oral bioavailability and brain permeability. In BAC transgenic mice containing a G2019S Parkinson's disease mutant that expresses human LRRK2 protein, GNE-0877 inhibited LRRK2 Ser1292 autophosphorylation in vivo. In vivo, GNE-0877 showed good oral bioavailability and brain permeability. In BAC transgenic mice containing a G2019S Parkinson's disease mutant that expresses human LRRK2 protein, GNE-0877 inhibited LRRK2 Ser1292 autophosphorylation in vivo. |
2-Methyl-2-(3-methyl-4-((4-(methylamino)-5-(trifluoromethyl)-pyrimidin-2-yl)amino)-1H-pyrazol- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.947 ml | 14.735 ml | 29.471 ml |
| 5 mM | 0.589 ml | 2.947 ml | 5.894 ml |
| 10 mM | 0.295 ml | 1.474 ml | 2.947 ml |
| 5 mM | 0.059 ml | 0.295 ml | 0.589 ml |
Last Update：2024-01-02 23:10:35
2-Methyl-2-(3-methyl-4-((4-(methylamino)-5-(trifluoromethyl)-pyrimidin-2-yl)amino)-1H-pyrazol- - Introduction
GNE-0877 (also known as Ro5059814) is a compound that belongs to the treatment of non-small cell lung cancer. It is a small molecule compound with a specific chemical structure. GNE-0877 interfere with the growth and spread of tumor cells primarily by inhibiting specific enzymatic activities.
The primary use of GNE-0877 is in the treatment of EGFR-positive non-small cell lung cancer. It can inhibit tumor growth by blocking specific signaling pathways within cancer cells by targeting the kinase activity of variable kinase domain mutations.
Preparation method, the synthesis of GNE-0877 can be divided into multiple steps. First, according to the needs of the chemical reaction, select the appropriate starting material, through different reaction steps to prepare the target compound. It is necessary to control the reaction time, temperature and amount of reactants in the synthesis to ensure high yield and purity.
When using GNE-0877, you need to pay attention to some safety information. It is a drug that must be used according to the doctor's instructions. During use, adverse reactions may occur, such as nausea, vomiting, fatigue, diarrhea, etc. Sometimes there are more serious adverse reactions, such as skin reactions and respiratory problems. Therefore, patients must be carefully evaluated for safety and tolerability before use, and follow the recommendations and warnings of doctors.
The primary use of GNE-0877 is in the treatment of EGFR-positive non-small cell lung cancer. It can inhibit tumor growth by blocking specific signaling pathways within cancer cells by targeting the kinase activity of variable kinase domain mutations.
Preparation method, the synthesis of GNE-0877 can be divided into multiple steps. First, according to the needs of the chemical reaction, select the appropriate starting material, through different reaction steps to prepare the target compound. It is necessary to control the reaction time, temperature and amount of reactants in the synthesis to ensure high yield and purity.
When using GNE-0877, you need to pay attention to some safety information. It is a drug that must be used according to the doctor's instructions. During use, adverse reactions may occur, such as nausea, vomiting, fatigue, diarrhea, etc. Sometimes there are more serious adverse reactions, such as skin reactions and respiratory problems. Therefore, patients must be carefully evaluated for safety and tolerability before use, and follow the recommendations and warnings of doctors.
Last Update：2024-04-09 21:48:26
Supplier List
Product Name: GNE-0877 Visit Supplier Webpage Request for quotation
CAS: 1374828-69-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1374828-69-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Product Name: GNE-0877 Visit Supplier Webpage Request for quotation
CAS: 1374828-69-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1374828-69-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History