 COA |
MSDS |
 HPLC |
NMR |
| CAS No: | 202590-98-5 |
| Molecular formula(MF) | C25H22ClN5O2S |
| Molecular Weight(MW): | 491.99 |
| Alias |
| In vitro | DMSO | 98 mg/mL (199.19 mM) |
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| Ethanol | 98 mg/mL (199.19 mM) | |
| Water | <1 mg/mL | |
| In vivo | 2% DMSO+30% PEG 300+5% Tween 80+ddH2O | 5mg/mL |
| Description | OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Phase 1. | ||||||||||||||||
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| Features | Orally bioavailable BRD2/3/4-selective inhibitor that has been tested in Phase I clinical trials for treatment of Haematological Malignancies. | ||||||||||||||||
| Targets |
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| In vitro |
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. [1] 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. [2] |
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| Cell Data |
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| In vivo | 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. [1] |