- EAI-045
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- $9.80 / 1.79999995231628KG
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2020-01-09
- CAS:1942114-09-1
- Min. Order: 1g
- Purity: ≥99%
- Supply Ability: 100kg
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| | EAI-045 Basic information |
| Product Name: | EAI-045 | | Synonyms: | 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) | | CAS: | 1942114-09-1 | | MF: | C19H14FN3O3S | | MW: | 383.4 | | EINECS: | | | Product Categories: | API;API | | Mol File: | 1942114-09-1.mol |  |
| | EAI-045 Chemical Properties |
| 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) |
| | EAI-045 Usage And Synthesis |
| 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 |
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