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Alternative_name
(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
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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%.
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CAS Number
202590-98-5
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Structure Available
Yes
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Salt Form
No
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Molecular Formula
C₂₅H₂₂ClN₅O₂S
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Molecular Weight
492
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Cell Permeable
Yes
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Purity
≥98%
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Solubilities
DMSO (~25 mg/ml) or EtOH (~ 25 mg/ml)
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Handling
Protect from air and light
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Tag Line
A bromodomain family inhibitor
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Storage Condition
-20°C
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Shipping Condition
gel pack
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Shelf Life
36 months
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PubChem CID
9936746
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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
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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
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InChi Key
GNMUEVRJHCWKTO-FQEVSTJZSA-N
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MSDS Available
Yes