ChemicalBook > CAS DataBase List > EAI-045

EAI-045

Product Name
EAI-045
CAS No.
1942114-09-1
Chemical Name
EAI-045
Synonyms
EA1045;EAI-045;CS-2350;EAI 045;EAI-045;EAI045;EAI 045;EAI-045;2-(5-fluoro-2-hydroxyphenyl)-2-(1-oxoisoindolin-2-yl)-N-(thiazol-2-yl)acetamide;α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-1-oxo-N-2-thiazolyl-2H-Isoindole-2-acetamide;α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-1-oxo-N-2-thiazolyl-2H-Isoindole-2-acetamide;2H-Isoindole-2-acetamide,α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-1-oxo-N-2-thiazolyl-;N-(3-((5-fluoroethoxy)phenyl)amino)pyrimidin-4-yl)amino)phenyl)acrylamide (EAI-045)
CBNumber
CB83122752
Molecular Formula
C19H14FN3O3S
Formula Weight
383.4
MOL File
1942114-09-1.mol
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EAI-045 Property

Density 
1.546±0.06 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
≥38.3 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
form 
solid
pka
7.20±0.50(Predicted)
color 
White to khaki
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
19719
Product name
EAI045
Purity
≥98%
Packaging
1mg
Price
$38
Updated
2024/03/01
Cayman Chemical
Product number
19719
Product name
EAI045
Purity
≥98%
Packaging
5mg
Price
$166
Updated
2024/03/01
Cayman Chemical
Product number
19719
Product name
EAI045
Purity
≥98%
Packaging
10mg
Price
$275
Updated
2024/03/01
Cayman Chemical
Product number
19719
Product name
EAI045
Purity
≥98%
Packaging
25mg
Price
$593
Updated
2024/03/01
TRC
Product number
F597850
Product name
α-​(5-Fluoro-​2-​hydroxyphenyl)​-​1,​3-​dihydro-​1-​oxo-​N-​2-​thiazolyl-2H-​isoindole-​2-​acetamide
Packaging
1mg
Price
$85
Updated
2021/12/16
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EAI-045 Chemical Properties,Usage,Production

Description

EAI045 is a potent and selective inhibitor of mutant EGF receptors (EGFRs; IC50s = 0.076, 0.049, 0.002, and 1.6 μM for recombinant EGFRL858R, EGFRT790M, EGFRL858R/T790M, and wild-type EGFR, respectively). It inhibits phosphorylation of EGFR in a concentration-dependent manner in H1975 cells. EAI045 (0.01-10 μM) reduces proliferation of Ba/F3 cells expressing EGFRL858R/T790M and EGFRL858R/T790M/I941R. In vivo, EAI045 induces tumor regression and reduces EGFR signaling in mice bearing EGFRL858R/T790M, EGFRExon19del/T790M, and EGFRL858R/T790M/C797S tumors when administered at a dose of 60 mg/kg per day in combination with cetuximab.

Description

EAI045 is a potent and selective EGFR inhibitor (fourth generation). EAI045 targets selected drug-resistant EGFR mutants without affecting the wild-type receptor. EAI045 inhibits L858R/T790M-mutant EGFR with low-nanomolar potency in biochemical assays. Therefore, it is a potential candidate drug for the treatment of related non-small cell lung cancer (NSCLC). It should be noted that EAI-045 is effectively in targeting the EGFR C797S mutation, which is resistance to the third-generation EGFR inhibitors including AZD9291 (osimertinib) and CO-1686 (rociletinib).

Uses

Epidermal growth factor receptor (EGFR) is a cell surface receptor often mutated in cancer cells. α-?(5-Fluoro-?2-?hydroxyphenyl)?-?1,?3-?dihydro-?1-?oxo-?N-?2-?thiazolyl-2H-?isoindole-?2-?acetamide is an allosteric EGFR inhibitor that is selective against drug-resistant EGFR mutants.

References

Wang, S., Y. Song, and D. Liu. "EAI045: The fourth-generation EGFR inhibitor overcoming T790M and C797S resistance." Cancer Letters385(2017):51.
Jia, Y., et al. "Overcoming EGFR T790M and C797S resistance with mutant-selective allosteric inhibitors:." Nature 534.7605(2016):129.

EAI-045 Preparation Products And Raw materials

Raw materials

Preparation Products

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EAI-045 Suppliers

China 126 India 1 United States 9 Global 136
A.J Chemicals
Tel
--
Fax
--
Email
sales@ajchem.in
Country
India
ProdList
6100
Advantage
58
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View Lastest Price from EAI-045 manufacturers

Career Henan Chemical Co
Product
EAI-045 1942114-09-1
Price
US $9.80/KG
Min. Order
1g
Purity
≥99%
Supply Ability
100kg
Release date
2020-01-08

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  • EAI-045
  • 2-(5-fluoro-2-hydroxyphenyl)-2-(1-oxoisoindolin-2-yl)-N-(thiazol-2-yl)acetamide
  • EA1045
  • α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-1-oxo-N-2-thiazolyl-2H-Isoindole-2-acetamide
  • EAI 045;EAI-045
  • CS-2350
  • EAI045;EAI 045;EAI-045
  • N-(3-((5-fluoroethoxy)phenyl)amino)pyrimidin-4-yl)amino)phenyl)acrylamide (EAI-045)
  • 2-(5-Fluoro-2-hydroxyphenyl)-2-(1-oxo-1,3-dihydro-2H-isoindol-2-yl)-N-1,3-thiazol-2-ylacetamide
  • 2H-Isoindole-2-acetamide, α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-1-oxo-N-2-thiazolyl-
  • 2H-Isoindole-2-acetamide,α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-1-oxo-N-2-thiazolyl-
  • α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-1-oxo-N-2-thiazolyl-2H-Isoindole-2-acetamide
  • 1942114-09-1
  • C19H14FN3O3S
  • API
  • API