Mavelertinib (Synonyms: PF-06747775) |
| Catalog No.GC61030 |
Mavelertinib es un inhibidor de la tirosina quinasa del EGFR (EGFR TKI) selectivo, disponible por vÍa oral e irreversible, con IC50 de 5, 4, 12 y 3 nM para Del, L858R y los mutantes dobles T790M/L858R y T790M/Del, respectivamente. Mavelertinib se puede utilizar para la investigaciÓn del cÁncer de pulmÓn de células no pequeÑas (NSCLC).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1776112-90-3
Sample solution is provided at 25 µL, 10mM.
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Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC)[1][2][3][4].
Mavelertinib exhibits selectivity over wild-type EGFR (IC50=307 nM)[1].Mavelertinib (10 μM) exhibits less than 50% e?ect or inhibition against all nonkinase targets[1].Mavelertinib inhibits the hERG26 current with an IC50 > 100 μM[1].
Mavelertinib exhibits low to moderate oral bioavailability (mouse 60%, rat 11%, dog 66%) following oral administration (mouse 1, rat 30, dog 3 mg/kg)[1].Mavelertinib exhibits short plasma half-lives (mouse 0.56, rat 0.28, dog 1.3 h) due to moderate to high plasma clearance (mouse 53, rat 49, dog 12 mL/min/kg) and low steady-state volume of distribution (mouse 1.48, rat 0.66, dog 0.94 L/kg) following intravenous administration (1 mg/kg to mouse, rat and dog)[1]. Animal Model: Female Nu/Nu mice[1]
[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 Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR. J Med Chem. 2017 Apr 13;60(7):3002-3019. [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.
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