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Submit ReviewAMG 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.
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 56.06 | 100 |
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.
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 |
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.
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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