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
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
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.
N-Bromosuccinimide Price
- Product number
- 19719
- Product name
- EAI045
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $38
- Updated
- 2024/03/01
- Product number
- 19719
- Product name
- EAI045
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $166
- Updated
- 2024/03/01
- Product number
- 19719
- Product name
- EAI045
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $275
- Updated
- 2024/03/01
- Product number
- 19719
- Product name
- EAI045
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $593
- Updated
- 2024/03/01
- 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
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
EAI-045 Suppliers
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- 18908622922
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- Country
- China
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- 86-21-57758967
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- (86) 21-58955996
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- QQ：3154870176
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View Lastest Price from EAI-045 manufacturers
- Product
- EAI-045 1942114-09-1
- Price
- US $9.80/KG
- Min. Order
- 1g
- Purity
- ≥99%
- Supply Ability
- 100kg
- Release date
- 2020-01-08