2. MAPK/ERK Pathway GPCR/G Protein Stem Cell/Wnt Apoptosis
  3. Ras ERK Apoptosis
  4. 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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K20 Chemical Structure

K20 Chemical Structure

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K20 Related Antibodies

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Description

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[1].

IC50 & Target

KRAS(G12C)

1.16 μM (IC50)

In Vitro

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.

K20 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: H358, H23, HCT116, A549, Pancl, Hela, SW620 cells
Concentration:
Incubation Time: 24 h
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).

Apoptosis Analysis[1]

Cell Line: NCI-H358 cells
Concentration: 0, 0.5, 2 µM
Incubation Time: 24 h
Result: Induced apoptosis of NCI-H358 cells.

Western Blot Analysis[1]

Cell Line: NCI-H358 cells
Concentration: 0, 0.5, 1.0, 2.5, 5.0 µM
Incubation Time: 48 h
Result: Decreased pErk (phosphorylated Erk) levels in NCI-H358 cells.
In Vivo

K20 (35 mg/kg; i.p.; every other day for 14 days) shows high tumor suppressive effects with a tumor growth inhibition (TGI) of 41% at 35 mg/kg[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-week-old male BALB/c nude mice ( xenograft model)[1]
Dosage: 35 mg/kg (dissolved in a 5%:35%:60% ratio of DMSO: castor oil: normal saline solution)
Administration: i.p.; every other day; 14 days
Result: Showed high tumor suppressive effects with a tumor growth inhibition (TGI) of 41% at 35 mg/kg.
Molecular Weight

543.34

Formula

C24H20Cl2F4N4O2
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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K20 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

K20K 20K-20RasERKApoptosisExtracellular signal regulated kinasesxenograft modelanticancerselectiveNCI-H358 cellsapoptosisInhibitorinhibitorinhibit

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