Description
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.
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
Additional Information
Storage Condition: |
-20°C |
Shipping Condition: |
Gel Pack |
Shelf Life: |
36 months |