1. GPCR/G Protein
    Apoptosis
  2. Ras
    Apoptosis
  3. K20

K20 

Cat. No.: HY-115907
Handling Instructions

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.

For research use only. We do not sell to patients.

K20 Chemical Structure

K20 Chemical Structure

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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[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].

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

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.

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].

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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K20
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