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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to light brown
溶解度
DMSO: 20 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
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 密鑰
GNMUEVRJHCWKTO-FQEVSTJZSA-N
基因資訊
human ... BRD2(6046) , BRD3(8019) , BRD4(23476) , BRDT(676)
生化/生理作用
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).
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Bromodomain inhibitor OTX015 in patients with acute leukaemia: a dose-escalation, phase 1 study.
The Lancet. Haematology, 3(4) (2016)
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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