EAI-045
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- CAS-Nr.
- 1942114-09-1
- Englisch Name:
- EAI-045
- Synonyma:
- 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
- Summenformel:
- C19H14FN3O3S
- Molgewicht:
- 383.4
- MOL-Datei:
- 1942114-09-1.mol
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EAI-045 Eigenschaften
- Dichte
- 1.546±0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C
- L?slichkeit
- ≥38.3 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
- Aggregatzustand
- solid
- pka
- 7.20±0.50(Predicted)
- Farbe
- White to khaki
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Bildanzeige (GHS) |
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| Alarmwort |
Warnung |
| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H302 |
Gesundheitssch?dlich bei Verschlucken. |
Akute Toxizit?t oral |
Kategorie 4 |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P270, P301+P312, P330, P501 |
| H315 |
Verursacht Hautreizungen. |
Hautreizung |
Kategorie 2 |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P280, P302+P352, P321,P332+P313, P362 |
| H319 |
Verursacht schwere Augenreizung. |
Schwere Augenreizung |
Kategorie 2 |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P280, P305+P351+P338,P337+P313P |
| H335 |
Kann die Atemwege reizen. |
Spezifische Zielorgan-Toxizit?t (einmalige Exposition) |
Kategorie 3 (Atemwegsreizung) |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
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| Sicherheit |
| P261 |
Einatmen von Staub vermeiden. |
| P305+P351+P338 |
BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen. |
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EAI-045 Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
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).
Verwenden
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.
Einzelnachweise
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 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
EAI-045 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 134)Lieferanten
- 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
