K20 是一种有效的选择性KRas G12C抑制剂，IC50为 1.16 μM。K20 在 H358 细胞中显示出抗癌活性（IC50= 0.78 μM）。K20 降低 ERK 的磷酸化水平并导致癌细胞凋亡 (Apoptosis)。K20 可抑制 NCI-H358 肿瘤细胞生长，TGI为 41%，且未引起明显毒性。

K20 is a potent and selective KRas G12C inhibitor with an IC 50 of 1.16 μM. K20 shows anticancer activity in H358 cells (IC 50 = 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].

K20 (24 h) shows selective cytotoxicity (5 to 23-fold) against KRas G12C mutated cells (H358, IC 50 =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]. 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, IC 50 =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.

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]. 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.

C24H20Cl2F4N4O2

543.34

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years