Osimertinib

• Description:

  Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].

• Product Name Alternative:

  AZD-9291; Mereletinib

• 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/AZD-9291.html

• Purity:

  99.99

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• Smiles:

  C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O

• Molecular Formula:

  C28H33N7O2

• Molecular Weight:

  499.61

• Precautions:

  H302, H315, H319, H335

• References & Citations:

  [1]Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4 (9) :1046-61.|[2]Hirano T, et al. Pharmacological and Structural Characterizations of Naquotinib, a Novel Third-Generation EGFR Tyrosine Kinase Inhibitor, in EGFR-Mutated Non-Small Cell Lung Cancer. Mol Cancer Ther. 2018 Apr;17 (4) :740-750.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• Isoform:

  EGFR/ErbB1/HER1

• Citation 01:

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• CAS Number:

  [1421373-65-0]