EAI045

• Description :

  EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFRL858R, EGFRT790M and EGFRL858R/T790M at 10 μM ATP, respectively.

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H312, H332

• 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/EAI045.html

• Purity :

  99.06

• Solubility :

  DMSO : 100 mg/mL (ultrasonic)

• Smiles :

  O=C(C(C1=C(O)C=CC(F)=C1)N2C(C(C=CC=C3)=C3C2)=O)NC4=NC=CS4

• Molecular Formula :

  C19H14FN3O3S

• Molecular Weight :

  383.40

• Precautions :

  H302, H312, H332

• References & Citations :

  [1]Jia Y, et al. Overcoming EGFR (T790M) and EGFR (C797S) resistance with mutant-selective allosteric inhibitors. Nature. 2016 Jun 2;534 (7605) :129-32.|[2]Wang S, et al. EAI045: The fourth-generation EGFR inhibitor overcoming T790M and C797S resistance. Cancer Lett. 2017 Jan 28;385:51-54.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

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

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  EGFR/ErbB1/HER1

• CAS Number :

  [1942114-09-1]