Antibodies
SCH772984
- 貨號 Cat. No.
- S7101
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
SCH772984
Catalog No.S7101
SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 of 4 nM and 1 nM, respectively.
| Availability |
|---|
The item is temporarily out of stock. Please leave your email address and we will inform you when we have it in stock. Just click the Arrival Notice and leave your email address to get 10% off. Arrival Notice |
Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 of 4 nM and 1 nM, respectively. | |||||
|---|---|---|---|---|---|---|
| Targets | ERK1 | ERK2 | ||||
| IC50 | 4 nM | 1 nM [1] | ||||
| In vitro | SCH772984 is a novel, selective and ATP competitive inhibitor of ERK1/2. SCH772984 inhibits phosphorylation of the ERK substrate p90 ribosomal S6 kinase (T359/S363 phospho-RSK) in a dose-dependent manner. SCH772984 also inhibits phosphorylation of residues in the activation loop of ERK itself. SCH772984 demonstrates EC50 values <500 nM in approximately 88% and 49% of BRAF-mutant or RAS-mutant tumor lines, respectively. Importantly, SCH772984 effectively inhibited MAPK signaling and cell proliferation in tumor cells resistant to concurrent treatment with BRAF and MEK inhibitors. [1] | |||||
| In vivo | SCH772984 induces tumor regressions in xenograft models at tolerated doses. SCH772984 effectively inhibites MAPK signaling and cell proliferation in BRAF or MEK inhibitor resistant models. [1] | |||||
| Features | Does not directly inhibit MEK1, MEK2, BRAF, or CRAF enzyme activity. | |||||
Protocol(Only for Reference)
Kinase Assay: [1]
| ERK2 IMAP enzymatic assay | SCH772984 is tested in 8 point dilution curves in duplicate against purified ERK2 or ERK1. The enzyme is added to the reaction plate. and incubated with the compound before adding a solution of substrate peptide and ATP. 14μl of diluted enzyme (0.3ng active ERK2 per reaction) is added to each well of a 384-well plate. The plates are gently shaken to mix the reagents and incubated for 45 minutes at room temperature. The reaction is stopped with 60μl of IMAP Binding Solution (1:2200 dilutions of IMAP beads in 1X Binding Buffer). The plates are incubated at room temperature for an additional 0.5 hours to allow complete binding of phosphopeptides to the IMAP beads. Plates are read on the LJL Analyst. |
|---|
Cell Assay: [1]
| Cell lines | BRAF-mutant or RAS-mutant tumor lines |
|---|---|
| Concentrations | ~10 μM |
| Incubation Time | 5 days |
| Method | Cell proliferation experiments are performed in a 96-well format (six replicates), and cells are plated at 4,000/well density. At 24 h after cell seeding, cells are treated with DMSO or 9 point IC50 dilution (0.001-10 μM) at 1% DMSO final for all concentrations. Viability is assayed on 5 days after dosing using ViaLight luminescence kit following the manufacturer’s recommendations. For cell line panel viability assay, cells are treated with SCH772984 for 4 days and assayed by CellTiterGlo luminescent cell viability assay. |
Animal Study: [1]
| Animal Models | Nude mice |
|---|---|
| Dosages | 12.5 mg/kg, 25 mg/kg, 50 mg/kg |
| Administration | i.p. |
References
Chemical Information
| Molecular Weight (MW) | 587.67 |
|---|---|
| Formula | C33H33N9O2 |
| CAS No. | 942183-80-4 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | mg/mL (<1 mM) |
|---|---|---|---|
| Water | mg/mL (<1 mM) | ||
| Ethanol | mg/mL (<1 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | (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 |
|---|
