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.
For research use only. We do not sell to patients.
- Formula: C28H29F3N6O5S
- Molecular Weight:618.63
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All MEK Isoforms
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Biological Activity
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MEK1 28 nM (IC50) |
Braf 3 nM (IC50) |
BRafV600E 3 nM (IC50) |
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Cell Line
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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
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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
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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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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)