Mavelertinib

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].

Product Specifications

CAS Number

[1776112-90-3]

Product Name Alternative

PF-06747775

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

EGFR

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/mavelertinib.html

Concentration

10mM

Purity

99.34

Solubility

DMSO : 47.5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

C=CC(N[C@@H]1CN(C2=NC(NC3=CN(C)N=C3OC)=C4N=CN(C)C4=N2)C[C@H]1F)=O

Molecular Formula

C18H22FN9O2

Molecular Weight

415.42

Precautions

H302, H315, H319, H335

References & Citations

[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.