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SML1605

OTX015

≥98% (HPLC)

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

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About This Item

Empirical Formula (Hill Notation):
C25H22ClN5O2S
CAS Number:
202590-98-5
Molecular Weight:
491.99
NACRES:
NA.77
PubChem Substance ID:
329825491
UNSPSC Code:
12352200
MDL number:
MFCD26960949
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100
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Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to light brown

solubility

DMSO: 20 mg/mL, clear

storage temp.

2-8°C

SMILES string

O=C(NC(C=C1)=CC=C1O)C[C@H]2C3=NN=C(C)N3C(SC(C)=C4C)=C4C(C5=CC=C(Cl)C=C5)=N2

InChI

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

Gene Information

human ... BRD2(6046), BRD3(8019), BRD4(23476), BRDT(676)

Biochem/physiol Actions

OTX015 is a potent inhibitor of the BET bromodomain proteins 2, 3, and 4 (BRD2/3/4).
OTX015 is a potent inhibitor of the BET bromodomain proteins 2, 3, and 4.
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 Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000159598
0000137293
0000115187
0000109679

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Bromodomain inhibitor OTX015 in patients with acute leukaemia: a dose-escalation, phase 1 study.
Berthon C
The Lancet. Haematology, 3(4) (2016)
Yaping Wu et al.
Theranostics, 9(6), 1777-1793 (2019-05-01)
The bromodomain and extraterminal family members are epigenetic readers and transcriptional coactivators which are critically involved in various biological processes including tumorigenesis. BRD4 has been increasingly appreciated as a key oncogene and promising anticancer target. Here, we sought to characterize
Nana Chen et al.
Cell reports, 39(11), 110970-110970 (2022-06-16)
Analysis of The Cancer Genome Atlas and other published data of head and neck squamous cell carcinoma (HNSCC) reveals somatic alterations of the Hippo-YAP pathway in approximately 50% of HNSCC. Better strategies to target the YAP1 transcriptional complex are sought.
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