AMG 510

Pricing Availability   Qty
说明: Potent and selective KRASG12C inhibitor
别名: Sotorasib
化学名: (1R)-6-Fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-4-[(2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]pyrido[2,3-d]pyrimidin-2(1H)-one
纯度: ≥98% (HPLC)
说明书
引用文献
评论
文献 (4)
通路 (1)

生物活性 for AMG 510

AMG 510 is a potent and selective covalent KRASG12C inhibitor (IC50 = 90 nM). Also a potent inhibitor of phospho-ERK (IC50 = 68 nM). In an in vivo model of non-small cell lung cancer, AMG 510 causes regression of tumors, an increase in T-cell recruitment and a pro-inflammatory tumor microenvironment. Synergises with MEK inhibitors and Carboplatin (Cat. No. 2626) and is orally bioavailable.

技术数据 for AMG 510

分子量 560.6
公式 C30H30F2N6O3
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2252403-56-6
PubChem ID 137278711
InChI Key NXQKSXLFSAEQCZ-SFHVURJKSA-N
Smiles O=C(C=C)N1C[C@H](C)N(C2=NC(N(C3=C(C)C=CN=C3C(C)C)C4=NC(C5=C(O)C=CC=C5F)=C(F)C=C42)=O)CC1

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for AMG 510

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 56.06 100

制备储备液 for AMG 510

以下数据基于产品分子量 560.6。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 1.78 mL 8.92 mL 17.84 mL
5 mM 0.36 mL 1.78 mL 3.57 mL
10 mM 0.18 mL 0.89 mL 1.78 mL
50 mM 0.04 mL 0.18 mL 0.36 mL

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参考文献 for AMG 510

参考文献是支持产品生物活性的出版物。

Lanman et al (2020) Discovery of a covalent inhibitor of KRASG12C (AMG 510) for the treatment of solid tumors. J.Med.Chem. 63 52 PMID: 31820981

Canon et al (2019) The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity. Nature 575 217 PMID: 31666701


If you know of a relevant reference for AMG 510, please let us know.

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查看全部 Ras GTPase Inhibitors

关键词: AMG 510, AMG 510 supplier, AMG510, KRASG12C, potent, selective, inhibitors, ERK, pERK, NSCLC, non, small, cell, lung, cancer, MEK, KRAS, G12C, Sotorasib, Ras, GTPases, 7713, Tocris Bioscience

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该领域的文献

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。


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Pathways for AMG 510

Akt Signaling Pathway

Akt Signaling Pathway

The Akt signaling pathway plays a key role in the mediation of protein synthesis, metabolism, proliferation and cell cycle progression. It may be referred to as a 'prosurvival' pathway.
MAPK Signaling Pathway

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.