K20
K20 is a potent and selective KRas G12C inhibitor with an IC50 of 1.16 µM. K20 shows anticancer activity in H358 cells (IC50= 0.78 µM). K20 decreases the levels of phosphorylated Erk and leads to cancer cell apoptosis. K20 suppresses NCI-H358 tumor growth with a TGI of 41% without causing obvious toxicity.
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- Fòrmula: C24H20Cl2F4N4O2
- Peso molecular:543.34
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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KRAS(G12C) 1.16 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| NCI-H23 | IC50 |
1.55 μM
Compound: 13
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Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant assessed as inhibition of cell growth
Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant assessed as inhibition of cell growth
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[PMID: 36680986] |
| NCI-H358 | IC50 |
0.78 μM
Compound: 13
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Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as inhibition of cell growth
Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as inhibition of cell growth
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[PMID: 36680986] |
K20 (24 h) shows selective cytotoxicity (5 to 23-fold) against KRas G12C mutated cells (H358, IC50=0.78 µM) over other KRas mutant (e.g.G12D, G12D, G12S, G12V) cancer cells (IC50s of 6.34, 17.74, 4.78, 5.03, 4.05 µM in HCT116 (G13D), A549 (G12S), Pancl (G12D), Hela (WT), SW620 (G12V), respectively)[1].
K20 (0, 0.5, 2 µM; 24 h) induces apoptosis of NCI-H358 cells[1].
K20 (0, 0.5, 1.0, 2.5, 5.0 µM; 48 h) decreases pErk (phosphorylated Erk) levels in NCI-H358 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H358, H23, HCT116, A549, Pancl, Hela, SW620 cells
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Concentration:
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Incubation Time:24 h
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Result:Showed selective cytotoxicity (5 to 23-fold) against KRas G12C mutated cells (H358, IC50=0.78 µM) over other KRas mutant (e.g.G12D, G12D, G12S, G12V) cancer cells (IC50s of 6.34, 17.74, 4.78, 5.03, 4.05 µM in HCT116 (G13D), A549 (G12S), Pancl (G12D), Hela (WT), SW620 (G12V), respectively).
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Cell Line:NCI-H358 cells
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Concentration:0, 0.5, 2 µM
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Incubation Time:24 h
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Result:Induced apoptosis of NCI-H358 cells.
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Cell Line:NCI-H358 cells
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Concentration:0, 0.5, 1.0, 2.5, 5.0 µM
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Incubation Time:48 h
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Result:Decreased pErk (phosphorylated Erk) levels in NCI-H358 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-week-old male BALB/c nude mice ( xenograft model)[1]
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Dosage:35 mg/kg (dissolved in a 5%:35%:60% ratio of DMSO: castor oil: normal saline solution)
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Administration:i.p.; every other day; 14 days
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Result:Showed high tumor suppressive effects with a tumor growth inhibition (TGI) of 41% at 35 mg/kg.
Chemical Information
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Peso molecular 543.34
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Fòrmula C24H20Cl2F4N4O2
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SMILES
C=C(C(N1CCN([C@@H](C1)C)C2=NC=NC3=C(C(C4=CC(Cl)=CC=C4OC)=C(C=C23)Cl)F)=O)C(F)(F)F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
K20 Related Classifications
HY-115907 Related Classifications
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