Orelabrutinib Struktur

Orelabrutinib

Bezeichnung:Orelabrutinib

CAS-Nr1655504-04-3

Englisch Name:Orelabrutinib

CBNumberCB03369553

SummenformelC26H25N3O3

Molgewicht427.49

MOL-Datei1655504-04-3.mol

Orelabrutinib physikalisch-chemischer Eigenschaften

Siedepunkt	646.3±55.0 °C(Predicted)
Dichte	1.213±0.06 g/cm3(Predicted)
Aggregatzustand	Solid
pka	14.80±0.50(Predicted)
Farbe	White to off-white

Gefahreninformationscode (GHS)

Orelabrutinib Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Orelabrutinib is a small molecule inhibitor of Bruton's tyrosine kinase with potential antineoplastic activity.
Beschreibung
In December 2020, orelabrutinib was approved by the China National Medical Products Administration for treating patients with relapsed/refractory MCL, CLL, and SLL. This compound is also being evaluated for the treatment of multiple sclerosis. Orelabrutinib, which has a unique pyridylcarboxamide hinge binder, showed an IC50 value of 1.6 nM in the BTK enzymatic assay. When tested against a panel of 456 kinases at 1 μM, orelabrutinib only inhibited BTK (>90%), while ibrutinib also targeted several other kinases, including EGFR, TEC, and BMX. Orelabrutinib has a favorable half-life of 4 h in healthy volunteers.1,2 It is administered orally at a daily dose of 150 mg.
Verwenden
Orelabrutinib has been previously approved to treat patients with relapsed or refractory (R/R) mantle cell lymphoma and R/R chronic lymphocytic leukemia/small lymphocytic lymphoma.
Trademarks
Innobruka^TM
Allgemeine Beschreibung
Class: non-receptor tyrosine kinase
Treatment: CLL, SLL, MCL
Elimination half-life = 4 h
Protein binding = not reported
Biologische Aktivität
Orelabrutinib (ICP-022) is a potent, orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK).
Mechanism of action
Upon administration, orelabrutinib binds to and inhibits the activity of BTK. This prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK.

target

Orelabrutinib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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Target	Value
BTK ()