Apabetalone
Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC50s are 87 μM and 0.51 μM for BD1 and BD2, respectively[1].
Product Specifications
CAS Number
1044870-39-4
Product Name Alternative
RVX-208; RVX000222
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Epigenetic Reader Domain; HIV
Type
Reference compound
Related Pathways
Anti-infection; Epigenetics
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/RVX-208.html
Purity
99.34
Solubility
DMSO : ≥ 33 mg/mL
Smiles
COC1=CC(OC)=C(C(NC(C2=CC(C)=C(OCCO)C(C)=C2)=N3)=O)C3=C1
Molecular Formula
C20H22N2O5
Molecular Weight
370.40
Precautions
H302, H315, H319, H335
References & Citations
[1]Picaud S, et al. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc Natl Acad Sci U S A. 2013 Dec 3;110 (49) :19754-9.|[2]McLure KG, et al. RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist. PLoS One. 2013 Dec 31;8 (12) :e83190.|[3]Jahagirdar R, et al. A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice. Atherosclerosis. 2014 Sep;236 (1) :91-100.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Available Sizes
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