OTX015

OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4. Phase 1. (In Vitro) :Birabresib (OTX-015) (500 nM) exposure induces a strong decrease of BRD2, BRD4 and c-MYC and increase of HEXIM1 proteins, while BRD3 expression is unchanged. c-MYC, BRD2, BRD3, BRD4 and HEXIM1 mRNA levels do correlate however with viability following exposure to Birabresib (OTX-015) . Birabresib (OTX-015) (0.1, 1, 5 μM) treatment induces HIV-1 full-length transcripts and viral outgrowth in resting CD4+ T cells from infected individuals receiving suppressive antiretroviral therapy (ART), while exerting minimal toxicity and effects on T cell activation. Birabresib-mediated activation of HIV-1 involves an increase in CDK9 occupancy and RNAP II C-terminal domain (CTD) phosphorylation. (In Vivo) :In MDA-MB-231 murine xenografts, tumor mass is significantly (p < 0.05) reduced by Birabresib (OTX-015) (50 mg/kg) with respect to vehicle-treated animals. Birabresib (OTX-015) in combination with 2 mg/kg RAD001 shows more effective activity than Birabresib alone.

202590-98-5

HY-15743 | (?) -OTX015

>98% (HPLC)

DMSO:98 mg/mL (199.19 mM) ; Ethanol:98 mg/mL (199.19 mM) ; Water:<1 mg/mL (<1 mM)

O=C (NC1=CC=C (O) C=C1) C[C@H]2C3=NN=C (C) N3C4=C (C (C) =C (C) S4) C (C5=CC=C (Cl) C=C5) =N2

C25H22ClN5O2S

491.99

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.