OTX015 Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, play a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-
dependent chromatin complexes. OTX015 is an orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC
50s = 10-
19 nM). It displays antiproliferative effects at a sub-
micromolar range
in vitro in a wide range of solid tumor types and leukemias, downregulating c-
Myc expression and inducing cell cycle arrest and apoptosis. At 100 mg/kg, OTX015 has been shown to inhibit the growth of Ty82 BRD-
NUT midline carcinoma tumors in nude mice by 79%.
Verwenden
(S)-2-(4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-hydroxyphenyl)acetamide is an orally bioavailable, inhibitor of BRD2, BRD3, and BRD4 to AcH4 and shows anti-tumor activity in vitro and in vivo tumor models.
Biochem/physiol Actions
It binds to bromodomain and extra-terminal domain (BET) proteins and inhibits their binding to the chromatin. This in turn prevents gene transcription. OTX015 has been shown to inhibit proliferation of cells in haematological malignancies.
OTX015 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
