Bioactivity | 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]. |
Invitro | 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]. Cell Cytotoxicity Assay[1] Cell Line: |
Name | K20 |
Formula | C24H20Cl2F4N4O2 |
Molar Mass | 543.34 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |