ERK2 IN-1
ERK2 IN-1 is a selective ERK2 inhibitor with an IC50 of 7 nM.
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- CAS No.: 1093061-47-2
- Formule: C36H34FN7O2S
- Masse moléculaire:647.76
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[1]|
ERK2 7 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COLO 205 | IC50 |
45 nM
Compound: 7
|
Antiproliferative activity against human COLO205 cells harboring BRAF V600E/D mutant measured after 4 days
Antiproliferative activity against human COLO205 cells harboring BRAF V600E/D mutant measured after 4 days
|
[PMID: 30034615] |
| HT-29 | IC50 |
118 nM
Compound: 7
|
Antiproliferative activity against human HT-29 cells harboring BRAF V600E/D mutant measured after 4 days
Antiproliferative activity against human HT-29 cells harboring BRAF V600E/D mutant measured after 4 days
|
[PMID: 30034615] |
| HT-29 | IC50 |
118 nM
Compound: 28
|
Antiproliferative activity against human HT-29 cells harboring BRAF/KRAS mutant
Antiproliferative activity against human HT-29 cells harboring BRAF/KRAS mutant
|
[PMID: 29748051] |
| HT-29 | IC50 |
80 nM
Compound: 28
|
Induction of apoptosis in human HT-29 cells harboring BRAF/KRAS mutant by caspase activation assay
Induction of apoptosis in human HT-29 cells harboring BRAF/KRAS mutant by caspase activation assay
|
[PMID: 29748051] |
In Vitro
ERK1/2 IN-1 (Compound 28) maintains good ERK enzymatic activity (ERK IC50=7 nM) and cellular activity in BRAF/KRAS mutant wildtype cancer cell lines (HT-29/Caspase IC50=118/80 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 1093061-47-2
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Masse moléculaire 647.76
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Formule C36H34FN7O2S
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SMILES
FC1=CC=C(C2=NNC3=C2C=C(NC([C@@]4(SC)CN(CC(N5CCC(C6=CC=C(C7=NC=CC=N7)C=C6)=CC5)=O)CC4)=O)C=C3)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)