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;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);2H-Isoindole-2-acetamide, α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-1-oxo-N-2-thiazolyl-
- CBNumber:
- CB83122752
- Molecular Formula:
- C19H14FN3O3S
- Molecular Weight:
- 383.4
- MDL Number:
- MFCD30187871
- MOL File:
- 1942114-09-1.mol
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P305+P351+P338 | |||||||||
| NFPA 704 |
|
EAI-045 price More Price(28)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 19719 | EAI045 ≥98% | 1942114-09-1 | 1mg | $38 | 2024-03-01 | Buy |
| Cayman Chemical | 19719 | EAI045 ≥98% | 1942114-09-1 | 5mg | $166 | 2024-03-01 | Buy |
| Cayman Chemical | 19719 | EAI045 ≥98% | 1942114-09-1 | 10mg | $275 | 2024-03-01 | Buy |
| Cayman Chemical | 19719 | EAI045 ≥98% | 1942114-09-1 | 25mg | $593 | 2024-03-01 | Buy |
| TRC | F597850 | α-(5-Fluoro-2-hydroxyphenyl)-1,3-dihydro-1-oxo-N-2-thiazolyl-2H-isoindole-2-acetamide | 1942114-09-1 | 1mg | $85 | 2021-12-16 | Buy |
EAI-045 Chemical Properties,Uses,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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Nanjing Gold Pharmaceutical Technology Co. Ltd. | 025-84209270 15906146951 | CHINA | 115 | 55 | |
| Beijing Cooperate Pharmaceutical Co.,Ltd | 010-60279497 | sales01@cooperate-pharm.com | CHINA | 1811 | 55 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| Zhejiang ZETian Fine Chemicals Co. LTD | 18957127338 | stella@zetchem.com | China | 2141 | 58 |
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 967 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| Jurong Coupling Biotechnology Co., Ltd. | 13656108824 | coupling278191416@hotmail.com | CHINA | 184 | 58 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
| ANHUI WITOP BIOTECH CO., LTD | +8615255079626 | eric@witopchemical.com | China | 23556 | 58 |
| AFINE CHEMICALS LIMITED | 0571-85134551 | info@afinechem.com | CHINA | 15377 | 58 |
