R428
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- CAS-Nr.
- 1037624-75-1
- Englisch Name:
- R428
- Synonyma:
- R428;CS-1130;BGB-324;EOS-62006;Bemcetinib;Bemcentinib;R428 (BGB324);BGB324 (R428);R428 USP/EP/BP;BGB-324, CPDB1725
- CBNumber:
- CB42621146
- Summenformel:
- C30H34N8
- Molgewicht:
- 506.64
- MOL-Datei:
- 1037624-75-1.mol
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R428 Eigenschaften
- Schmelzpunkt:
- >211°C (dec.)
- Siedepunkt:
- 799.6±70.0 °C(Predicted)
- Dichte
- 1.41±0.1 g/cm3(Predicted)
- storage temp.
- -20°C
- L?slichkeit
- Soluble in DMSO (up to at least 25 mg/ml)
- Aggregatzustand
- Yellow powder.
- pka
- 10.34±0.20(Predicted)
- Farbe
- Yellow
- Stabilit?t:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
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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R428 Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
R428 (bemcentinib, BGB324), a selective small-molecule inhibitor of AXL, is currently being evaluated in phase II trials for the treatment of non-small-cell lung cancer (NSCLC) and acute myelocytic leukemia (AML). It has been found to induce apoptosis in cancer cells and to block tumor spread in models of metastatic breast cancer. The therapeutic potential of R428 has also been demonstrated in highly invasive esophageal adenocarcinoma cells and in ESCC cells.
R428 is a selective, small molecule inhibitor of Axl that blocks its catalytic and precancerous activities. R428 treatment reduced Axl-induced AKT phosphorylation, cancer cell invasion, angiogenesis, and the production of pro-inflammatory cytokines. It also reduced the expression of the cytokine granulocyte macrophage colony-stimulating factor and Snail in a dosage-dependent manner. Interestingly,using R428 to inhibit Axl-mediated cellular and molecular functions during cisplatin treatments achieved an enhanced suppression of liver metastases. Axl knockdowns in RAC cell lines reduced migration, invasion, and in vivo engraftment, accompanied by a downregulation in the activity of the Ral GTPase proteins (RalA and RalB). Similar effects were obtained using an A428 inhibitor. Blocking Axl functions also abrogated the phosphorylation of ERBB2 (Her-2/neu) at the Tyr877 residue, which reveals the cross-functional effects of R428 on different receptor signaling axes.
Cabozantinib (XL184) and R428 (BGB324) Inhibit the Growth of Esophageal Squamous Cell Carcinoma (ESCC)
Verwenden
R 428 is an AXL tyrosine kinase inhibitor shown to be used as an anti-cancer agent.
R428 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
R428 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 163)Lieferanten
- (S)-1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)-1H-1,2,4-triazole-3,5-diamine
- BGB-324
- BGB-324, CPDB1725
- (S)-1-(6,7-Dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8
- R428
- R428 (BGB324)
- 1-(6,7-Dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-[(7S)-6,7,8,9-tetrahydro-7-(1-pyrrolidinyl)-5H-benzocyclohepten-2-yl]-1H-1,2,4-triazole-3,5-diamine
- BGB324(R428,Bemcentinib)
- 1-(6,7-dihydro-5H-benzo[2,3]cyclohepta[2,4-d]pyridazin-3-yl)-3-N-[(7S)-7-pyrrolidin-1-yl-6,7,8,9-tetrahydro-5H-benzo[7]annulen-3-yl]-1,2,4-triazole-3,5-diamine
- R428-(R) (R428-P1)
- CS-1130
- Bemcentinib(R428,BGB324)
- R-428; R 428;BGB-324;BGB 324
- BEMCENTINIB (R428)
- 1H-1,2,4-Triazole-3,5-diamine, 1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-[(7S)-6,7,8,9-tetrahydro-7-(1-pyrrolidinyl)-5H-benzocyclohepten-2-yl]-
- R428 USP/EP/BP
- Bemcentinib intermediate
- EOS-62006
- Bemcentinib
- BGB324 (R428)
- R428, 98%, a potent and selective inhibitor of Axl
- Bemcentinib BGB-324 R428
- (S)-1-(6,7-Dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-[7-(1-pyrrolidinyl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl]-1H-1,2,4-triazole-3,5-diamine
- Bemcentinib Crude
- R-428 (BEMCENTINIB)
- R428 (BGB324), AXL inhibitor
- Bemcetinib
- 1037624-75-1
- C30H34N8
- C31H35N7
- Inhibitors
- APIs
- API
