Pyrido[2,3-d]pyrimidin-2(1H)-one, 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-4-[(2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-, (1R)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one
Pyrido[2,3-d]pyrimidin-2(1H)-one, 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-4-[(2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-, (1R)-
CAS: 2296729-00-3
Molecular Formula: C30H30F2N6O3
Pyrido[2,3-d]pyrimidin-2(1H)-one, 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-4-[(2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-, (1R)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one - Names and Identifiers
Pyrido[2,3-d]pyrimidin-2(1H)-one, 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-4-[(2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-, (1R)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one - Physico-chemical Properties
| Molecular Formula | C30H30F2N6O3 |
| Molar Mass | 560.61 |
| Density | 1.36±0.1 g/cm3(Predicted) |
| Boling Point | 730.5±70.0 °C(Predicted) |
| pKa | 6.52±0.35(Predicted) |
| Storage Condition | -20℃ |
| Physical and Chemical Properties | Bioactive Sotorasib (AMG510) is a potent covalent inhibitor of KRAS G12C with potential antitumor activity. The AMG510 is a chiral compound. |
| In vitro study | AMG 510 inhibited the nucleotide exchange of the recombinant mutant KRAS (G12C/C118A) catalyzed by SOS1, but had little effect on the single mutant KRAS (C118A). AMG 510 selectively reduced the viability of cell lines containing the KRAS p.G12C mutation, but had no effect on cell lines containing other KRAS mutations. |
| In vivo study | In preclinical tumor models, AMG 510 rapidly and irreversibly binds to KRAS (G12C), permanently inhibiting the MAPK signaling pathway. AMG 510 was able to induce tumor regression in a mouse tumor model containing KRAS(G12C) mutations by a single administration by the oral route. |
Pyrido[2,3-d]pyrimidin-2(1H)-one, 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-4-[(2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-, (1R)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.784 ml | 8.919 ml | 17.838 ml |
| 5 mM | 0.357 ml | 1.784 ml | 3.568 ml |
| 10 mM | 0.178 ml | 0.892 ml | 1.784 ml |
| 5 mM | 0.036 ml | 0.178 ml | 0.357 ml |
Last Update：2024-01-02 23:10:35
Pyrido[2,3-d]pyrimidin-2(1H)-one, 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-4-[(2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-, (1R)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one - Uses and synthesis methods
target
Target Value
K-Ras(G12C)
in vitro study
AMG 510 inhibits the nucleotide exchange of SOS1-catalyzed recombinant mutant KRAS (G12C/C118A), but has little effect on single mutant KRAS (C118A). AMG 510 selectively reduced the viability of cell lines containing KRAS p.G12C mutations, but had no effect on cell lines containing other KRAS mutations.
in vivo studies
In preclinical tumor models, AMG 510 can quickly bind KRAS (G12C) in an irreversible manner, and permanently inhibit MAPK signaling pathway. For mouse tumor models containing KRAS(G12C) mutations, AMG 510 can induce tumor regression by single oral administration.
Last Update：2024-04-10 22:29:15
![Pyrido[2,3-d]pyrimidin-2(1H)-one, 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-4-[(2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-, (1R)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one](http://res.chembk.com/assets/images/structure/1000484.png)
Supplier List
Spot supply
Product Name: rac Sotorasib Visit Supplier Webpage Request for quotationCAS: 2296729-00-3
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: AMG-510 Visit Supplier Webpage Request for quotationCAS: 2296729-00-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: rac Sotorasib Visit Supplier Webpage Request for quotationCAS: 2296729-00-3
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: AMG-510 Visit Supplier Webpage Request for quotationCAS: 2296729-00-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History