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HomeProduct name listOTX015

OTX015

Synonym(s):6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-N-(4-hydroxyphenyl)-2,3,9-trimethyl-, (6S)-;OTX-015

OTX015 Structural

What is OTX015?

Description

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 (EC50s = 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%.

The Uses of OTX015

(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.

Definition

ChEBI: 6h-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-n-(4-hydroxyphenyl)-2,3,9-trimethyl-, (6s)- is an organonitrogen heterocyclic compound and an organosulfur heterocyclic compound.

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.

storage

Store at -20°C

Properties of OTX015

Melting point: 220 °C
Density  1.45±0.1 g/cm3(Predicted)
storage temp.  2-8°C
solubility  ≥24.6 mg/mL in DMSO; insoluble in H2O; ≥106 mg/mL in EtOH with gentle warming
pka 10.05±0.26(Predicted)
form  powder
color  white to light brown

Safety information for OTX015

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for OTX015

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