OTX 015 化学特性,用途語,生産方法
外観
白色～うすい黄色～うすい黄赤色粉末～結晶
効能
抗悪性腫瘍薬
説明
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%.
使用
(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.
OTX 015 上流と下流の製品情報
原材料
準備製品