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SML1605

Sigma-Aldrich

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
MDL number:
MFCD26960949
UNSPSC Code:
12352200
PubChem Substance ID:
329825491
NACRES:
NA.77

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

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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

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