ERK2-IN-6
ERK2-IN-6 (Compound 20) is a highly selective ERK1/2 inhibitor with an IC50 value of 7.9 nM for ERK2. ERK2-IN-6 inhibits the proliferation of BRAFV600E mutant cells (IC50=250 nM in A375 cells). ERK2-IN-6 is promising for research of solid tumors, such as BRAF-mutated melanoma.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 2095713-33-8
- Formel: C28H30ClN5O3
- Molecular Weight:520.02
-
Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
|
ERK1 |
ERK2 7.9 nM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
250 nM
Compound: 20
|
Antiproliferative activity against human A375 cells harboring BRAF V600E mutant after 96 hrs by Alamar blue assay
Antiproliferative activity against human A375 cells harboring BRAF V600E mutant after 96 hrs by Alamar blue assay
|
[PMID: 29775310] |
| COLO 205 | IC50 |
310 nM
Compound: 20
|
Antiproliferative activity against human COLO205 cells harboring BRAF V600E mutant after 96 hrs by Alamar blue assay
Antiproliferative activity against human COLO205 cells harboring BRAF V600E mutant after 96 hrs by Alamar blue assay
|
[PMID: 29775310] |
Chemical Information
-
CAS. Nr. 2095713-33-8
-
Molecular Weight 520.02
-
Formel C28H30ClN5O3
-
SMILES
O=C1C2=C(CN1CC(NC(C)(C)C3=CC=CC=C3)=O)C=CC(C4=NC(NC5CCOCC5)=NC=C4Cl)=C2
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)