(3S)-3-(2-Chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-ylamino)-N-isopropylpyrrolidine-1-carboxamide
NVS-PAK1-1
CAS: 1783816-74-9
Molecular Formula: C23H25ClF3N5O
(3S)-3-(2-Chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-ylamino)-N-isopropylpyrrolidine-1-carboxamide - Names and Identifiers
(3S)-3-(2-Chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-ylamino)-N-isopropylpyrrolidine-1-carboxamide - Physico-chemical Properties
| Molecular Formula | C23H25ClF3N5O |
| Molar Mass | 479.93 |
| Density | 1.42±0.1 g/cm3(Predicted) |
| Boling Point | 697.8±55.0 °C(Predicted) |
| Solubility | DMSO: ≥125 mg/mL |
| Appearance | powder |
| Color | white to beige |
| pKa | 14.02±0.40(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | NVS-PAK1-1 demonstrates high selectivity for inhibition of PAK1 over other PAK isoforms and the kinome in general. NVS-PAK1-1 has a biochemical PAK1 K d of 7 nM and a PAK2 K d of 400 nM. NVS-PAK1-1 shows excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases. NVS-PAK1-1 at 6-20 μM inhibits the phosphorylation of the downstream substrate MEK1 Ser289. Consistent with the observation, NVS-PAK1-1 inhibits proliferation of Su86.86 cell line only above a concentration of 2 μM. In contrast, by applying a mixture of NVS-PAK1-1 and PAK2 shRNA, inhibition of downstream signaling and cell proliferation at a significantly lower 0.21 μM concentration are achieved. |
| In vivo study | NVS-PAK1-1 shows a relatively poor stability in rat liver microsomes (RLM) and this would limit its application for in vivo studies (t 1/2 in RLM 3.5 min). |
(3S)-3-(2-Chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-ylamino)-N-isopropylpyrrolidine-1-carboxamide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.084 ml | 10.418 ml | 20.837 ml |
| 5 mM | 0.417 ml | 2.084 ml | 4.167 ml |
| 10 mM | 0.208 ml | 1.042 ml | 2.084 ml |
| 5 mM | 0.042 ml | 0.208 ml | 0.417 ml |
Last Update：2024-01-02 23:10:35
(3S)-3-(2-Chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-ylamino)-N-isopropylpyrrolidine-1-carboxamide - Introduction
NVS-PAK1-1 is a chemical compound, which is a peptide compound that selectively inhibits the activation of P21-kinase.
The use of NVS-PAK1-1 is as an experimental tool in biomedical research to study the function and regulation mechanism of p21-kinase. P21-kinase plays an important regulatory role in cells, and is involved in the regulation of a variety of cellular processes and signal transduction pathways. NVS-PAK1-1 can selectively inhibit p21-kinase activity, helping researchers understand the kinase's role in biological processes.
The production method of NVS-PAK1-1 is generally obtained by chemical synthesis. The specific synthesis method may vary depending on the research institutions and experimental conditions.
Regarding the safety information of the NVS-PAK1-1, because it is an experimental tool, it is generally used in a laboratory environment and should follow the relevant safety operation procedures. Avoid direct contact with skin and eyes during operation, ensure that the laboratory is well ventilated, and avoid inhaling compound gases or dust. At the same time, for research projects using NVS-PAK1-1, relevant experimental safety guidelines should be followed and government and legal regulations should be followed. When using NVS-PAK1-1, you should pay attention to personal protection to avoid adverse effects on the human body and the environment. In any experiment or work that uses chemical substances, the laboratory's safe operating procedures should be followed to ensure personal and environmental safety.
The use of NVS-PAK1-1 is as an experimental tool in biomedical research to study the function and regulation mechanism of p21-kinase. P21-kinase plays an important regulatory role in cells, and is involved in the regulation of a variety of cellular processes and signal transduction pathways. NVS-PAK1-1 can selectively inhibit p21-kinase activity, helping researchers understand the kinase's role in biological processes.
The production method of NVS-PAK1-1 is generally obtained by chemical synthesis. The specific synthesis method may vary depending on the research institutions and experimental conditions.
Regarding the safety information of the NVS-PAK1-1, because it is an experimental tool, it is generally used in a laboratory environment and should follow the relevant safety operation procedures. Avoid direct contact with skin and eyes during operation, ensure that the laboratory is well ventilated, and avoid inhaling compound gases or dust. At the same time, for research projects using NVS-PAK1-1, relevant experimental safety guidelines should be followed and government and legal regulations should be followed. When using NVS-PAK1-1, you should pay attention to personal protection to avoid adverse effects on the human body and the environment. In any experiment or work that uses chemical substances, the laboratory's safe operating procedures should be followed to ensure personal and environmental safety.
Last Update：2024-04-09 21:54:55
![(3S)-3-(2-Chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-ylamino)-N-isopropylpyrrolidine-1-carboxamide](http://res.chembk.com/assets/images/structure/HY-100519.gif)
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Product Name: NVS-PAK1-1 Visit Supplier Webpage Request for quotation
CAS: 1783816-74-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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CAS: 1783816-74-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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