MEK/RAF-IN-1
MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC50 values of 28 nM for MEK1, and 3 nM each for BRAF and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer.
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- Formel: C28H29F3N6O5S
- Molecular Weight:618.63
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
|
MEK1 28 nM (IC50) |
Braf 3 nM (IC50) |
BRafV600E 3 nM (IC50) |
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| H9c2 | IC50 |
>50 μM
Compound: 16b
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Antiproliferative activity against rat H9c2 cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against rat H9c2 cells incubated for 72 hrs by CCK8 assay
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[PMID: 39166848] |
| HCT-116 | IC50 |
0.079 μM
Compound: 16b
|
Antiproliferative activity against human HCT-116 cells harboring KRAS G13D mutant incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human HCT-116 cells harboring KRAS G13D mutant incubated for 72 hrs by CCK8 assay
|
[PMID: 39166848] |
| HeLa | IC50 |
>10 μM
Compound: 16b
|
Antiproliferative activity against human HeLa cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human HeLa cells incubated for 72 hrs by CCK8 assay
|
[PMID: 39166848] |
| MIA PaCa-2 | IC50 |
0.011 μM
Compound: 16b
|
Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant incubated for 72 hrs by CCK8 assay
|
[PMID: 39166848] |
Chemical Information
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Molecular Weight 618.63
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Formel C28H29F3N6O5S
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SMILES
FC1=C(NC2=C(F)C=C(C3CC3)C=C2)C(C(NOCCO)=O)=CC4=C1N=CN4CC5=C(F)C(NS(=O)(NCC)=O)=CC=C5
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)