OTX015 202590-98-5

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Molecular Weight:

491.99 OTX015 is a potent Bet Bromodomain Inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4. Phase 1.


Biological Activity


OTX015 inhibits the binding of BRD2, BRD3, and BRD4 to AcH4 with IC50
ranging from 92 to 112 nM, and inhibits the growth of a variety of human
cancer cell lines with GI50 ranging from 60 to 200 nM. OTX015 results in rapid down-regulation of c-MYC expression, and show
the synergistic anti-proliferative effects in combination with ALK
Inhibitors in ALKpos ALCL cell lines.


OTX015 (p.o.) significantly inhibits the growth of Ty82 BRD-NUT midline
carcinoma tumors in nude mice by 79% at 100 mg/kg qd and 61% at 10 mg/kg
bid, respectively.


TR-FRET Assay

To assess binding of OTX015 to BRD2, BRD3, and BRD4, BRD-expressing CHO
cell lysate (from CHO cells transfected with expression plasmids for
Flag-tagged BRD2, BRD3, or BRD4 or vector alone), europium-conjugated
anti-Flag antibody, XL-665-conjugated streptavidin, and biotinylated
OTX015 are incubated at room temperature for 0.2 to 2 h. Fluorescence is
measured by TR-FRET using an EnVision 2103 Multilabel Reader and EC50
for binding is calculated by nonlinear regression using PRISM version
5.02.

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Product Categories : Epigenetics > Epigenetic Reader Domain Inhibitor