OTX015 | 2651

OTX015 is a potent 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%.

OTX015 is a potent 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.

2651 | OTX015 DataSheet

Alternate Name/Synonyms: (6S)-​4-​(4-​chlorophenyl)-​N-​(4-​hydroxyphenyl)-​2,​3,​9-​trimethyl-​6H-​thieno[3,​2-​f][1,​2,​4]triazolo[4,​3-​a][1,​4]diazepine-​6-​acetamide; HY-15743

Appearance: Crystaline solid

Formulation: N/A

CAS Number: 202590-98-5

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₅H₂₂ClN₅O₂S

Molecular Weight: 492

Cell-Permeable?: Yes

Purity: ≥98%

Solubilities: DMSO (~25 mg/ml) or EtOH (~ 25 mg/ml)

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A bromodomain family inhibitor

MDL Number: N/A

PubChem CID: 9936746

SMILES: CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NC4=CC=C(C=C4)O)C5=CC=C(C=C5)Cl)C

InChi: nChI=1S/C25H22ClN5O2S/c1-13-14(2)34-25-22(13)23(16-4-6-17(26)7-5-16)28-20(24-30-29-15(3)31(24)25)12-21(33)27-18-8-10-19(32)11-9-18/h4-11,20,32H,12H2,1-3H3,(H,27,33)/t20-/m0/s1

InChi Key: GNMUEVRJHCWKTO-FQEVSTJZSA-N