Welcome to ProbeChem!Global Supplier of Chemical Probes, Inhibitors & Agonists.
EN | CN

You are here:Home-Chemical Inhibitors & Agonists-Tyrosine Kinase-EGFR-EAI-045
EAI-045

Chemical Structure : EAI-045

CAS No.: 1942114-09-1

EAI-045 (EAI045)

Catalog No.: PC-42087Not For Human Use, Lab Use Only.

EAI-045 (EAI045) is a potent, mutant-selective allosteric EGFR inhibitor with IC50 of 3 nM for double mutant L858R/T790M in biochemical assays at 1 mM ATP.

Packing Price Stock Quantity
25 mg $158 In stock
50 mg $248 In stock
100 mg $398 In stock
200 mg Get quote
1 g Get quote

Bulk size, bulk discount!

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

EAI-045 (EAI045) is a potent, mutant-selective allosteric EGFR inhibitor with IC50 of 3 nM for double mutant L858R/T790M in biochemical assays at 1 mM ATP.
EAI-045 (EAI045) displays >1000-fold selectivity versus wild type EGFR, also inhibits L858R and T790M with IC50 of 76 and 49 nM.
EAI-045 (EAI045) potently inhibits EGFR Y1173 phosphorylation in H1975 cells (EC50=2 nM).
EAI-045 (EAI045) exhibits true mechanistic synergy combined with cetuximab in mouse models of lung cancer driven by EGFR(L858R/T790M) and by EGFR(L858R/T790M/C797S).

Physicochemical Properties

M.Wt 383.3961
Formula C19H14FN3O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 28 mg/mL

Chemical Name/SMILES

2H-Isoindole-2-acetamide, α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-1-oxo-N-2-thiazolyl-

References

1. Jia Y, et al. Nature. 2016 Jun 2;534(7605):129-32.

2. Wang S, et al. J Hematol Oncol. 2016 Jul 22;9(1):59.

Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright

Contact Us sales@probechem.com

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • *Additional Information:

Get Quote

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • Additional Information: