Fruquintinib
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- CAS-Nr.
- 1194506-26-7
- Englisch Name:
- Fruquintinib
- Synonyma:
- CS-1643;R-228060;HMPL-013;EOS-61054;BMS-986472;Fruquintinib;Fruquintinib|HMPL-013;Fruquintinib Impurity;Fruquintinib, 10 mM in DMSO;Fruquintinib|HMPL-013 USP/EP/BP
- CBNumber:
- CB23037638
- Summenformel:
- C21H19N3O5
- Molgewicht:
- 393.39
- MOL-Datei:
- 1194506-26-7.mol
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Fruquintinib Eigenschaften
- Siedepunkt:
- 600.5±55.0 °C(Predicted)
- Dichte
- 1.302±0.06 g/cm3(Predicted)
- storage temp.
- Sealed in dry,Store in freezer, under -20°C
- L?slichkeit
- Soluble in DMSO (up to 5 mg/ml).
- pka
- 14.35±0.46(Predicted)
- Aggregatzustand
- solid
- Farbe
- White
- Stabilit?t:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
- InChI
- InChI=1S/C21H19N3O5/c1-11-19(20(25)22-2)13-6-5-12(7-16(13)28-11)29-21-14-8-17(26-3)18(27-4)9-15(14)23-10-24-21/h5-10H,1-4H3,(H,22,25)
- InChIKey
- BALLNEJQLSTPIO-UHFFFAOYSA-N
- SMILES
- O1C2=CC(OC3=C4C(=NC=N3)C=C(OC)C(OC)=C4)=CC=C2C(C(NC)=O)=C1C
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 |
src="/GHS07.jpg" width="20" height="20" /> |
P264, P270, P301+P312, P330, P501 |
H315 |
Verursacht Hautreizungen. |
Hautreizung |
Kategorie 2 |
Warnung |
src="/GHS07.jpg" width="20" height="20" /> |
P264, P280, P302+P352, P321,P332+P313, P362 |
H319 |
Verursacht schwere Augenreizung. |
Schwere Augenreizung |
Kategorie 2 |
Warnung |
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 |
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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Fruquintinib Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Fruquintinib is a VEGFR inhibitor (IC
50s = 33, 35, and 0.5 nM for VEGFR1, -2, and -3, respectively). It also inhibits RET, FGFR1, and c-Kit (IC
50s = 128, 181, and 458 nM, respectively) in a panel of 253 kinases. Fruquintinib inhibits VEGF-A-induced proliferation of human umbilical vein endothelial cells (HUVECs) and VEGF-C-induced proliferation of human lymphatic endothelial cells (HLECs; IC
50s = 1.7 and 4.2 nM, respectively). It decreases tube formation by HUVECs by 74 and 94% when used at concentrations of 30 and 300 nM, respectively. Fruquintinib (0.5-20 mg/kg per day for 21 days) reduces tumor growth in BGC-823, HT-29, Caki-1, and NCI H460 mouse xenograft models.
Verwenden
Fruquintinib (HMPL-013) is a highly selective VEGFR-1/2/3 tyrosine kinase inhibitor. It was approved by the FDA on 8 November 2023 for the treatment of adult patients with metastatic colorectal cancer. and these patients had previously received fluoropyrimidine, oxaliplatin and irinotecan chemotherapy, anti-vascular endothelial growth factor therapy, and anti-epidermal growth factor receptor (EGFR) therapy. Fruquintinib has also been shown to improve cognitive deficits and pathological changes in a mouse model of cerebral amyloid angiopathy (CAA).
Verwenden
Fruquintinib is a multi-targeted tyrosine kinase inhibitor, a third-line regimen involved in the treatment of advanced non-small cell lung cancer in humans. Fruquintinib is a potent, highly selective and orally active inhibitor of VEGFR1, 2, 3 tyrosine kinases.
Trademarks
Fruzaqla
Fruquintinib Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
Fruquintinib Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 221)Lieferanten
- Fruquintinib|HMPL-013
- Fruquintinib
- 6-(6,7-dimethoxyquinazolin-4-yloxy)-N,2-dimethylbenzofuran-3-carboxamide
- HMPL-013
- 3-Benzofurancarboxamide, 6-[(6,7-dimethoxy-4-quinazolinyl)oxy]-N,2-dimethyl-
- 6-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-N,2-dimethyl-3-benzofurancarboxamide
- R-228060
- 6-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-N,2-dimethyl-1-benzofuran-3-carboxamide
- Fruquintinib|HMPL-013 USP/EP/BP
- EOS-61054
- CS-1643
- BMS-986472
- Fruquintinib, 10 mM in DMSO
- Fruquintinib Impurity
- 1194506-26-7
- Inhibitors
- API