K20

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

K20 

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

K20 Chemical Structure

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生物活性

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)

体外研究
(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].

上海金畔生物科技有限公司 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.

体内研究
(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].

上海金畔生物科技有限公司 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.

分子量

543.34

Formula

C24H20Cl2F4N4O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

  • [1]. Zhao H, et al. Discovery of ARS-1620 analogs as KRas G12C inhibitors with high in vivo antitumor activity. Bioorg Chem. 2022, 121:105652.

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