(R)-1-(2-oxo-2-(4-(4-(pyrimidin-2-yl)phenyl)piperazin-1-yl)ethyl)-N-(3-(pyridin-4-yl)-1H-indazol-5-yl)pyrrolidine-3-carboxamide
SCH772984
CAS: 942183-80-4
Molecular Formula: C33H33N9O2
(R)-1-(2-oxo-2-(4-(4-(pyrimidin-2-yl)phenyl)piperazin-1-yl)ethyl)-N-(3-(pyridin-4-yl)-1H-indazol-5-yl)pyrrolidine-3-carboxamide - Names and Identifiers
(R)-1-(2-oxo-2-(4-(4-(pyrimidin-2-yl)phenyl)piperazin-1-yl)ethyl)-N-(3-(pyridin-4-yl)-1H-indazol-5-yl)pyrrolidine-3-carboxamide - Physico-chemical Properties
| Molecular Formula | C33H33N9O2 |
| Molar Mass | 587.67 |
| Density | 1.353±0.06(20.0000℃) |
| Melting Point | >214°C (dec.) |
| Boling Point | 857.3±65.0 °C(Predicted) |
| Solubility | DMSO (Slightly) |
| Appearance | Solid |
| Color | Pale Yellow |
| pKa | 12.05±0.40(Predicted) |
| Storage Condition | Refrigerator |
| In vitro study | SCH772984 is a novel, selective, ATP-competitive ERK1/2 inhibitor. SCH772984 inhibited the phosphorylation of the ERK substrate p90 ribosomal S6 kinase (T359/S363 phosphorylation-RSK) in a dose-dependent manner. SCH772984 also inhibits phosphorylation of residues in the activation loop of ERK itself. SCH772984 inhibited approximately 88% and 49% of the BRAF-mutant or RAS-mutant tumor cell lines, respectively, with EC50 values <500 nM. |
| In vivo study | SCH772984 treated the xenograft model at a tolerated dose to induce tumor regression. Sch 772984 acts on a model of anti-BRAF or MEK inhibitors, effectively inhibiting MAPK signaling and cell proliferation. |
(R)-1-(2-oxo-2-(4-(4-(pyrimidin-2-yl)phenyl)piperazin-1-yl)ethyl)-N-(3-(pyridin-4-yl)-1H-indazol-5-yl)pyrrolidine-3-carboxamide - Risk and Safety
| HS Code | 29339900 |
(R)-1-(2-oxo-2-(4-(4-(pyrimidin-2-yl)phenyl)piperazin-1-yl)ethyl)-N-(3-(pyridin-4-yl)-1H-indazol-5-yl)pyrrolidine-3-carboxamide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.702 ml | 8.508 ml | 17.016 ml |
| 5 mM | 0.34 ml | 1.702 ml | 3.403 ml |
| 10 mM | 0.17 ml | 0.851 ml | 1.702 ml |
| 5 mM | 0.034 ml | 0.17 ml | 0.34 ml |
Last Update：2024-01-02 23:10:35
(R)-1-(2-oxo-2-(4-(4-(pyrimidin-2-yl)phenyl)piperazin-1-yl)ethyl)-N-(3-(pyridin-4-yl)-1H-indazol-5-yl)pyrrolidine-3-carboxamide - Reference Information
| biological activity | SCH772984 is a novel specific inhibitor of ERK1/2, the IC50 in the cell-free assay is 4 nM and 1 nM, respectively, and has powerful efficacy against cancer cells containing RAS or BRAF mutations. |
| Target | Value |
| ERK2 (Cell-free assay) | 1 nM |
| ERK1 (Cell-free assay) | 4 nM |
Last Update：2024-04-09 21:11:58
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View History
(R)-1-(2-oxo-2-(4-(4-(pyrimidin-2-yl)phenyl)piperazin-1-yl)ethyl)-N-(3-(pyridin-4-yl)-1H-indazol-5-yl)pyrrolidine-3-carboxamide
4,12-Dihydro-11-[2-[N-(benzyloxycarbonyl)methylamino]ethyl]-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14-dione
2-Propenoic acid, 2-methyl-, C14-18-alkyl esters, C16-rich
Di(2-thienyl) persulfide
1-Acetyl-3-(4-chlorophenyl)-2-(2,4-dimethoxyphenyl)-2,3-dihydro-4(3H)-quinazolinone
3586-69-4
74299-34-6
4-chloro-1-(4-methylbenzyl)-1H-pyrazol-3-amine
1224885-25-9
4,12-Dihydro-11-[2-[N-(benzyloxycarbonyl)methylamino]ethyl]-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14-dione
2-Propenoic acid, 2-methyl-, C14-18-alkyl esters, C16-rich
Di(2-thienyl) persulfide
1-Acetyl-3-(4-chlorophenyl)-2-(2,4-dimethoxyphenyl)-2,3-dihydro-4(3H)-quinazolinone
3586-69-4
74299-34-6
4-chloro-1-(4-methylbenzyl)-1H-pyrazol-3-amine
1224885-25-9