EAI-045

ChemicalBook > CAS DataBase List > 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, 10 mM in DMSO;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;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 EGFR^L858R, EGFR^T790M, EGFR^L858R/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 EGFR^L858R/T790M and EGFR^{L858R/T790M/I941R}. In vivo, EAI045 induces tumor regression and reduces EGFR signaling in mice bearing EGFR^L858R/T790M, EGFR^{Exon19del/T790M}, and EGFR^{L858R/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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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-

EAI045, 10 mM in DMSO

1942114-09-1

C19H14FN3O3S

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