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Sotorasib(AMG-510)racemate
本半岛bd体育手机客户端 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。
Sotorasib(AMG-510)racemate图片
CAS NO: 2252403-56-6
规格: ≥98%
包装与价格:
包装 价格(元)
5mg 电议
10mg 电议
25mg 电议
50mg 电议
100mg 电议
250mg 电议
500mg 电议

半岛bd体育手机客户端 介绍
理化性质和储存条件


Molecular Weight: 560.59
Formula: C30H30F2N6O3
SMILES: O=C(C=C)N1C[C@H](C)N(C2=NC(N(C3=C(C)C=CN=C3C(C)C)C4=C2C=C(F)C(C5=C(O)C=CC=C5F)=N4)=O)CC1
Storage -20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Technical Information Synonym: AMG-510 racemate; AMG 510; AMG510; Sotorasib
实验参考方法

In Vitro: Sotorasib (AMG-510; 1-10 μM; 72 hours) also potently impairs cellular viability in both NCI-H358 and MIA PaCa-2 with IC50≈0.006 μM and 0.009 μM, respectively. Non-KRASG12C lines are insensitive to Sotorasib (IC50>7.5 μM) [1]; In cellular assays, Sotorasib (AMG-510) covalently modifies KRAS G12C and inhibits KRAS G12C signaling as measured by phosphorylation of ERK1/2 (p-ERK) in allKRAS p.G12C-mutant cell lines [2].

In Vivo: In animal tumor models, Sotorasib (AMG-510) rapidly and irreversibly binds to KRAS G12C, providing durable suppression of the mitogen-activated protein kinase (MAPK) signaling pathway. Sotorasib (orally; once daily) is capable of inducing tumor regression in mouse models of KRAS G12C cancer [2].

References:

[1]. Abstract 3090: In vivo characterization of AMG 510 - a potent and selective KRASG12Ccovalent small molecule inhibitor in preclinical KRASG12Ccancer models. Experimental and Molecular Therapeutics.

[2].The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity. Nature. 2019 Nov;575(7781):217-223.


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