DDR1-IN-2
|
|
|
- CAS-Nr.
- 1429617-90-2
- Englisch Name:
- DDR1-IN-2
- Synonyma:
- 7rh;DDR1-IN-2;DDR1 Inhibitor 7rh;DDR1 Inhibitor 7rh >=98% (HPLC);DDR1 IN 2,Discoidin Domain Receptor,Inhibitor,7rh,inhibit,DDR-1-IN-2,DDR1IN2;4-Ethyl-N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)-3-(pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamide;4-ETHYL-N-{3-[(4-METHYLPIPERAZIN-1-YL)METHYL]-5-(TRIFLUOROMETHYL)PHENYL-3-(2-{PYRAZOLO[1,5-A]PYRIMIDIN-6-YLETHYNYL)BENZAMIDE;Benzamide, 4-ethyl-N-[3-[(4-methyl-1-piperazinyl)methyl]-5-(trifluoromethyl)phenyl]-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)-
- CBNumber:
- CB53367620
- Summenformel:
- C30H29F3N6O
- Molgewicht:
- 546.59
- MOL-Datei:
- 1429617-90-2.mol
|
DDR1-IN-2 Eigenschaften
- storage temp.
- 2-8°C
- Löslichkeit
- DMSO: 62.5 mg/mL (114.35 mM)
- Aggregatzustand
- powder
- Farbe
- white to beige
Sicherheit
- Risiko- und Sicherheitserklärung
- Gefahreninformationscode (GHS)
| Bildanzeige (GHS) |
|
| Alarmwort |
Warnung |
| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H302 |
Gesundheitsschädlich bei Verschlucken. |
Akute Toxizität 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-Toxizität (einmalige Exposition) |
Kategorie 3 (Atemwegsreizung) |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
|
|
| 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 Möglichkeit entfernen. Weiter spülen. |
|
DDR1-IN-2 Chemische Eigenschaften,Einsatz,Produktion Methoden
Allgemeine Beschreibung
DDR1 Inhibitor 7rh is a small potent kinase inhibitor of discoidin domain receptor-1 (DDR1). It inhibits the tumorigenicity of nasopharyngeal carcinoma (NPC) cells. DDR1 Inhibitor 7rh prevents the proliferation, invasion and adhesion of cancer cells.
Biochem/physiol Actions
DDR1 Inhibitor 7rh is an orally available, potent, ATP-competitive DDR1-selective inhibitor with in vitro and in vivo anti-cancer efficacy. Compound 7rh is a potent, high affinity (Kd =0.6 nM), ATP-competitive inhibitor against discoidin domain-containing receptor 1 (DDR1; IC50 = 6.8 nM, [ATP] = 100 nM) with significantly reduced potency toward 455 other kinases, including DDR2, Bcr-abl, and c-Kit (IC50 = 101.4 nM, 355 nM and >10 μM, respectively). Inhibitor 7rh reduces DDR1 expression/phosphorylation and downstream signaling in a dose-dependent manner (0.1-2 μM; NCI-H23 NSCLCs), effectively suppressing human cancer cells proliferation (IC50 from 38 nM/K562 to 2.98 μM/NCI-H460) and colony formation (IC50 = 0.56 μM/NCI-H23). Inhibitor 7rh is orally availabe in rats and mice (T1/2 = 15.53 h; Tmax = 4.25 h; Cmax = 1867.5 μg/L, F = 67.4%; 25 mg/kg; rats) and displays in vivo efficacy against Kras (LSLG12Vgeo) tumor growth in mice (50 mg/kg/day p.o.).
DDR1-IN-2 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
DDR1-IN-2 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.
Global( 34)Lieferanten
- 4-Ethyl-N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)-3-(pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamide
- 4-ETHYL-N-{3-[(4-METHYLPIPERAZIN-1-YL)METHYL]-5-(TRIFLUOROMETHYL)PHENYL-3-(2-{PYRAZOLO[1,5-A]PYRIMIDIN-6-YLETHYNYL)BENZAMIDE
- DDR1-IN-2
- DDR1 Inhibitor 7rh
- Benzamide, 4-ethyl-N-[3-[(4-methyl-1-piperazinyl)methyl]-5-(trifluoromethyl)phenyl]-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)-
- DDR1 Inhibitor 7rh >=98% (HPLC)
- 7rh
- DDR1 IN 2,Discoidin Domain Receptor,Inhibitor,7rh,inhibit,DDR-1-IN-2,DDR1IN2
- 1429617-90-2
- C30H29F3N6O
