4-[4-Fluoro-3-[(4-methoxypiperidin-1-yl)carbonyl]benzyl]phthalazin-1(2H)-one
2-Pyrazinecarboxamide, 3-amino-6-[4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-N-3-pyridinyl-
CAS: 1174043-16-3
Molecular Formula: C22H22FN3O3
4-[4-Fluoro-3-[(4-methoxypiperidin-1-yl)carbonyl]benzyl]phthalazin-1(2H)-one - Names and Identifiers
4-[4-Fluoro-3-[(4-methoxypiperidin-1-yl)carbonyl]benzyl]phthalazin-1(2H)-one - Physico-chemical Properties
| Molecular Formula | C22H22FN3O3 |
| Molar Mass | 395.43 |
| Density | 1.33±0.1 g/cm3(Predicted) |
| Appearance | powder |
| Color | white to beige |
| pKa | 12.07±0.40(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | AZD2461 has a lower affinity for Pgp than Olaparib. |
| In vivo study | AZD2461 acts on KB1P tumor T6-28 against Olaparib, increasing the expression of Mdr1b by 80 times, and does not inhibit Pgp. Short-term treatment of mice bearing KB1P tumors with AZD2461 induced a loss of 53BP1 expression. AZD2461 was well tolerated with long-term treatment, and the mean relapse-free survival was doubled. |
4-[4-Fluoro-3-[(4-methoxypiperidin-1-yl)carbonyl]benzyl]phthalazin-1(2H)-one - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.529 ml | 12.644 ml | 25.289 ml |
| 5 mM | 0.506 ml | 2.529 ml | 5.058 ml |
| 10 mM | 0.253 ml | 1.264 ml | 2.529 ml |
| 5 mM | 0.051 ml | 0.253 ml | 0.506 ml |
Last Update：2024-01-02 23:10:35
4-[4-Fluoro-3-[(4-methoxypiperidin-1-yl)carbonyl]benzyl]phthalazin-1(2H)-one - Reference Information
| biological activity | AZD2461 is a new type of PARP inhibitor, which has lower affinity for Pgp than Olaparib. Phase 1. |
| target | TargetValue PARP |
| Target | Value |
| in vitro studies | AZD2461 acts on Pgp with lower affinity than Olaparib. |
| in vivo studies | AZD2461 act on anti-Olaparib KB1P tumor T6-28, increase Mdr1b expression by 80 times, and do not inhibit Pgp. AZD2461 short-term treatment of mice carrying KB1P tumor induced 53BP1 expression loss. AZD2461 long-term treatment, it is well tolerated, and the average relapse-free survival is doubled. |
Last Update：2024-04-09 21:54:55
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Spot supply
Product Name: 2-Pyrazinecarboxamide, 3-amino-6-[4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-N-3-pyridinyl- Visit Supplier Webpage Request for quotationCAS: 1174043-16-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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