2-Propen-1-one, 1-[4-[(7S)-6-chloro-8-fluoro-7-(2-fluoro-6-hydroxyphenyl)-4-quinazolinyl]-1-piperazinyl]-
ARS-1620
CAS: 1698055-85-4
Molecular Formula: C21H17ClF2N4O2
2-Propen-1-one, 1-[4-[(7S)-6-chloro-8-fluoro-7-(2-fluoro-6-hydroxyphenyl)-4-quinazolinyl]-1-piperazinyl]- - Names and Identifiers
2-Propen-1-one, 1-[4-[(7S)-6-chloro-8-fluoro-7-(2-fluoro-6-hydroxyphenyl)-4-quinazolinyl]-1-piperazinyl]- - Physico-chemical Properties
| Molecular Formula | C21H17ClF2N4O2 |
| Molar Mass | 430.84 |
| Density | 1.434±0.06 g/cm3(Predicted) |
| Boling Point | 614.7±55.0 °C(Predicted) |
| pKa | 6.03±0.35(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | In mutant p.G12C cancer cells, ARS-1620 covalently inhibited KRAS (G12C) activity with high potency and inhibition isomerization. ARS-1620 can rapidly occupy the G12C site in a concentration-dependent and time-dependent manner, exerting covalent inhibition. In cell lines containing this mutant allele, the TE50 value for target G12C ARS-1620 was approximately 0.3 μm. After 2 hours of 3 μm ARS-1620 treatment, the G12C was almost completely occupied. At H358 (p. In G12C) cells, ARS-1620 selectively inhibited phosphorylation of RAS-GTP and MEK, ERK, RSK, S6, and AKT in a concentration-dependent manner, but in the negative control group (lacking p.G12C lung cancer cell line; A549, H460 and H441 cells) did not have this activity. ARS-1620 is specific for the activity of the G12C allele, mediated by Cys-12 covalent modification. |
| In vivo study | In mice, ARS-1620 had good oral bioavailability with F>60%. In a MIA-PaCa2 xenograft model carrying the p.G12C mutation, ARS-1620 inhibited tumor growth in a concentration-dependent manner, with significant regression at a concentration of 200 mg/kg/day. In a patient-derived tumor model, ARS-1620 selectively induced tumor regression. In H441 (p.G12V) transplanted tumor, ARS-1620 had no effect. The ARS-1620 R-atropisomer had no active effect in either model. ARS-1620 selectively induces tumor regression in patient-derived xenografts (PDX) with KRAS p.G12C mutation. |
2-Propen-1-one, 1-[4-[(7S)-6-chloro-8-fluoro-7-(2-fluoro-6-hydroxyphenyl)-4-quinazolinyl]-1-piperazinyl]- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.321 ml | 11.605 ml | 23.21 ml |
| 5 mM | 0.464 ml | 2.321 ml | 4.642 ml |
| 10 mM | 0.232 ml | 1.161 ml | 2.321 ml |
| 5 mM | 0.046 ml | 0.232 ml | 0.464 ml |
Last Update：2024-01-02 23:10:35
2-Propen-1-one, 1-[4-[(7S)-6-chloro-8-fluoro-7-(2-fluoro-6-hydroxyphenyl)-4-quinazolinyl]-1-piperazinyl]- - Introduction
ARS-1620 is a chemical, the details of which are not yet known. Based on the information provided, it is not possible to accurately answer information about the nature, use, manufacture and safety of the ARS-1620. If you have more detailed information, I will be able to give a more accurate answer.
Last Update：2024-04-10 22:29:15
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Spot supply
Product Name: ARS-1620 Visit Supplier Webpage Request for quotationCAS: 1698055-85-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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