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SCH772984
| Product Name | SCH772984 |
| Price: | Inquiry |
| Catalog No.: | CN00501 |
| CAS No.: | 942183-80-4 |
| Molecular Formula: | C33H33N9O2 |
| Molecular Weight: | 587.67 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | O=C(N1CCN(CC1)c1ccc(cc1)c1ncccn1)CN1CC[C@H](C1)C(=O)Nc1ccc2c(c1)c(n[nH]2)c1ccncc1 |
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| Description | SCH772984 potently inhibits ERK1 and ERK2 activity with IC50s of 4 and 1 nM, respectively. |
| Target | ERK2:1 nM (IC50) ERK1:4 nM (IC50) |
| In Vitro | SCH772984 shows EC50 values less than 500 nM in approximately 88% and 49% of BRAF-mutant (n=25) or RAS-mutant (n=35) tumor lines, respectively. Flow cytometric analysis of SCH772984-sensitive melanoma cells revealed a G1 arrest as well as an increase in the sub-G1 fraction indicative of apoptosis. Less than 20% of cells wild-type for both RAS and BRAF (n=61) are sensitive to SCH772984[1]. |
| In Vivo | Treatment of BRAF-mutant LOX melanoma xenografts with SCH772984 (50 mg/kg twice daily) leads to 98% tumor regression. Dose-dependent antitumor activity is also observed in the KRAS-mutant pancreatic MiaPaCa model, with 36% regression at 50 mg/kg twice daily. Importantly, tumor regression is accompanied by robust inhibition of ERK phosphorylation in tumor tissue. SCH772984 is well tolerated on this schedule as measured by morbidity, lethality, or body weight loss[1]. |
| Cell Assay | Cell proliferation experiments are carried out in a 96-well format (six replicates), and the BRAFV600E-mutant human melanoma cell line LOXIMV1 (LOX) are plated at a density of 4,000 cells per well. At 24 hours after cell seeding, cells are treated with DMSO or a 9-point IC50 dilution (0.001-10 μM) at a final concentration of 1% DMSO for all concentrations. Viability is assayed 5 days after dosing using the ViaLight luminescence kit. For the cell line panel viability assay, cells are treated with SCH772984 for 4 days and assayed by the CellTiterGlo luminescent cell viability assay[1]. |
| Animal Admin | Mice[1] Nude mice are injected subcutaneously with specific cell lines, grown to approximately 100 mm3, randomized to treatment groups (10 mice/group), and treated intraperitoneally with either SCH772984 (12.5, 25, or 50 mg/kg) or vehicle. Tumor length (L), width (W), and height (H) are measured during and after the treatment periods by a caliper twice weekly on each mouse and then used to calculate tumor volume using the formula (L×W×H)/2. Animal body weights are measured on the same days twice weekly. Upon completion of the experiment, vehicle- and SCH772984-treated tumor biopsies are processed for Western blot analysis. |
| Density | 1.4±0.1 g/cm3 |
| Boiling Point | 857.3±65.0 °C at 760 mmHg |
| Flash Point | 472.3±34.3 °C |
| Exact Mass | 587.275696 |
| PSA | 126.73000 |
| LogP | 2.10 |
| Vapour Pressure | 0.0±3.2 mmHg at 25°C |
| Storage condition | -20℃ |