K20

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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。

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.