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K20
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
K20图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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。
生物活性

K20 is a potent and selectiveKRas G12Cinhibitor with anIC50of 1.16 μM. K20 shows anticancer activity in H358 cells (IC50= 0.78 μM). K20 decreases the levels of phosphorylatedErkand leads tocancercellapoptosis. K20 suppresses NCI-H358 tumor growth with aTGIof 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 (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: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.
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].

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.