SCH772984 HCl
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SCH772984 HCl is a specific inhibitor of extracellular signal-regulated kinase 1/2 (ERK1/2), with IC50 values of 4 nM and 1 nM, respectively [1].
ERK1/2 is a mitogen-activated protein kinase (MAPK) which is involved in the development of various cancers, especially the ones with BRAF or RAS mutations. Phospho-ERK reactivation in cancer cells is associated with resistance to BRAF and MEK inhibitors [1].
In BRAFV600E-mutant human melanoma cell line LOXIMV1 (LOX), SCH772984 at 0 ~ 300 nM inhibited phosphorylation of the ERK substrate p90 ribosomal S6 kinase in a dose-dependent manner. SCH772984 also reduced phosphorylation of residues in the activation loop of ERK itself. In addition, for approximately 88% and 49% of BRAF-mutant or RAS-mutant tumor lines, SCH772984 exhibited antiproliferative activity with EC50 values < 500 nM. SCH772984 effectively inhibited MAPK signaling and cell proliferation even in tumor cells resistant to concurrent treatment with BRAF and MAP-ERK kinase (MEK) inhibitors [1].
In female nude mice bearing human LOX BRAFV600E tumors, SCH772984 (12.5, 25, 50 mg/kg, i.p., b.i.d., for 14 days) induced tumor regressions in a dose-dependent manner, and 98% tumor regression was achieved at the largest dose [1].
Reference:
[1]. Morris E J, Jha S, Restaino C R, et al. Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors. Cancer Discovery, 2013, 3(7): 742-750.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 624.17 |
| Cas No. | 942183-80-4 (free base) |
| Formula | C33H34ClN9O2 |
| Solubility | ≥23.5 mg/mL in H2O with gentle warming; insoluble in EtOH; ≥16.27 mg/mL in DMSO |
| SDF | Download SDF |
| Canonical SMILES | O=C(N1CCN(C2=CC=C(C3=NC=CC=N3)C=C2)CC1)CN4CC[C@@](/C(O)=N/C5=CC(C(C6=CC=NC=C6)=NN7)=C7C=C5)([H])C4.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Cell experiment:[1] | |
|
Cell lines |
BRAFV600E-mutant human melanoma cell line LOXIMV1 (LOX) |
|
Reaction Conditions |
0 ~ 300 nM SCH772984 for 24 h incubation |
|
Applications |
SCH772984 inhibited phosphorylation of the ERK substrate p90 ribosomal S6 kinase in a dose-dependent manner. SCH772984 also reduced phosphorylation of residues in the activation loop of ERK itself, a modification catalyzed by the ERK-activating kinases, MEK 1 and MEK 2. |
| Animal experiment:[1] | |
|
Animal models |
Female nude mice bearing human LOX BRAFV600E tumors |
|
Dosage form |
12.5, 25, 50 mg/kg Twice daily (b.i.d.) by intraperitoneal route (i.p.) for 14 days |
|
Applications |
In female nude mice bearing human LOX BRAFV600E tumors, SCH772984 (12.5, 25, 50 mg/kg, i.p., b.i.d., for 14 days) induced tumor regressions in a dose-dependent manner, and 98% tumor regression was achieved at the largest dose. |
|
Note |
The technical data provided above is for reference only. |
|
References: 1. Morris E J, Jha S, Restaino C R, et al. Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors. Cancer Discovery, 2013, 3(7): 742-750. |
|
质量控制和MSDS
- 批次:
化学结构
