SML1605
OTX015
≥98% (HPLC)
别名:
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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关于此项目
经验公式（希尔记法）:
C25H22ClN5O2S
化学文摘社编号:
分子量:
491.99
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
产品名称
OTX015, ≥98% (HPLC)
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
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 key
GNMUEVRJHCWKTO-FQEVSTJZSA-N
assay
≥98% (HPLC)
form
powder
color
white to light brown
solubility
DMSO: 20 mg/mL, clear
storage temp.
2-8°C
Quality Level
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).
OTX015 is a potent inhibitor of the BET bromodomain proteins 2, 3, and 4.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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.
Leiming Wang et al.
The Journal of clinical investigation, 130(4), 1782-1792 (2019-12-25)
Recent findings have shown that inhibitors targeting bromodomain and extraterminal domain (BET) proteins, such as the small molecule JQ1, are potent growth inhibitors of many cancers and hold promise for cancer therapy. However, some reports have also revealed that JQ1
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