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Chemical Structure| 1942114-09-1 Chemical Structure| 1942114-09-1

Structure of EAI045
CAS No.: 1942114-09-1

Chemical Structure| 1942114-09-1

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CAS No.: 1942114-09-1

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EAI045, an allosteric inhibitor, selectively targets drug-resistant EGFR mutants like EGFR-L858R, EGFR-T790M and EGFR-L858R/T790M with IC50 of 0.019 μM, 0.19 μM and 0.002 μM respectively.

Synonyms: EAI045

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Product Details of EAI045

CAS No. :1942114-09-1
Formula : C19H14FN3O3S
M.W : 383.40
SMILES Code : O=C(NC1=NC=CS1)C(C2=CC(F)=CC=C2O)N(CC3=C4C=CC=C3)C4=O
Synonyms :
EAI045
MDL No. :MFCD30187871
InChI Key :YTUFHOKUFOQRDF-UHFFFAOYSA-N
Pubchem ID :121231412

Safety of EAI045

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of EAI045

RTK
JAK-STAT

Isoform Comparison

Biological Activity

Target
  • mutant EGFR

In Vitro:

Cell Line
Concentration Treated Time Description References
Ba/F3 cells 10 μM 72 hours Inhibited proliferation of L858R/T790M and L858R mutant cells PMC4929832
H3255 cells 163 nM 3 hours Intermediate level of EGFR inhibition PMC4929832
HaCaT cells >10 μM 3 hours Did not inhibit EGFR phosphorylation PMC4929832
H1975 cells 2 nM 3 hours Inhibited EGFR autophosphorylation but did not completely eliminate it PMC4929832
MDCK-II cells 5 μM 1, 2, 4, and 8 h To evaluate the transepithelial transport ability of EAI045 in MDCK-II cells, it was found that EAI045 is a good transport substrate of human ABCB1, with weak transport ability for mouse Abcg2 and human ABCG2. PMC9505538

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice L858R/T790M mutant lung cancer model Oral gavage 60 mg/kg Once daily for 4 weeks Combination with cetuximab induced marked tumor regression PMC4929832
Mice Wild-type (WT), Abcb1a/1b-/-, Abcg2-/-, Abcb1a/1b;Abcg2-/-, Oatp1a/1b-/-, Cyp3a-/-, and Cyp3aXAV mice Oral 20 mg/kg Single dose, observation times were 30 minutes, 4 hours, and 24 hours To evaluate the pharmacokinetics and tissue distribution of EAI045 in mice, it was found that Abcb1a/1b significantly limits brain accumulation of EAI045, while Abcg2 has a minor effect. Coadministration of elacridar can significantly enhance brain accumulation and oral exposure of EAI045. PMC9505538

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.04mL

2.61mL

1.30mL

26.08mL

5.22mL

2.61mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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