Mavelertinib

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Chemical Structure| 1776112-90-3 同义名 : PF-06747775
CAS号 : 1776112-90-3
货号 : A133482
分子式 : C18H22FN9O2
纯度 : 99%
分子量 : 415.42
MDL号 : MFCD29079007
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 Mavelertinib is a selective, orally bioavailable, irreversible inhibitor of EGFR tyrosine kinase (EGFR TKI), exhibiting IC50 values of 5, 4, 12, and 3 nM for Del, L858R, and the double mutants T790M/L858R and T790M/Del, respectively. It holds potential for research in non-small-cell lung cancer (NSCLC)[1][2][3][4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.04mL

2.41mL

1.20mL

24.07mL

4.81mL

2.41mL
参考文献

[1]Planken S, et, al. Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Onc

[2]Murtuza A, et, al. Novel Third-Generation EGFR Tyrosine Kinase Inhibitors and Strategies to Overcome Therapeutic Resistance in Lung Cancer. Cancer Res. 2019 Feb 15; 79(4): 689-698.

[3]Patel H, et, al. Recent updates on third generation EGFR inhibitors and emergence of fourth generation EGFR inhibitors to combat C797S resistance. Eur J Med Chem. 2017 Dec 15; 142:32-47.

[4]Husain H, et, al. First-in-human phase I study of PF-06747775, a third-generation mutant selective EGFR tyrosine kinase inhibitor (TKI) in metastatic EGFR mutant NSCLC after progression on a first-line EGFR TKI. Annals of Oncology. 2017 Sep.