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RVX-208

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Catalog: ASIS-P044

Formal Name: 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one

Produced By: AsisChem, Inc.

Biological Description

ASIS-P044 or RVX-208 is a potent inhibitor against the bromo and extraterminal (BET) proteins with selectivity for the second bromodomain BD2 (IC50 = 0.510 ?M) (Picaud et al. 2013 and McLure et al. 2013). Bromodomain (BRD) proteins bind to acetylated lysines of histones regulating gene expression and chromatin remodeling. The BET family of bromodomain proteins consists of BRD2, BRD3, BRD4, and BRDT. RVX-208 is currently undergoing clinical trials for the treatment of cardiovascular disease (CVD) (Bailey et al 2010 and Nicholls et al 2012). The drug is effective against CVD partly through its role in increasing apolipoprotein A-I (ApoA-1) expression levels by inhibiting BRD4 (McLure et al. 2013).

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Additional Information

Quantities Please contact us for larger or different quantities
Catalog ASIS-P044
Formal Name 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one
CAS Number RVX-208 is a potent BET bromodomain inhibitor
Molecular Weight 370.399078369141
Formula C20 H22 N2 O5
Lead Time 3
LogP No
Purity 95
SMILES C12C(=O)NC(C3=CC(C)=C(OCCO)C(C)=C3)=NC1=CC(OC)=CC=2OC
Solubility and Handling No
inchikey NETXMUIMUZJUTB-UHFFFAOYSA-N
TPSA No
HBD No
HBA No

Details

Picaud, S., C. Wells, I. Felletar, D. Brotherton, S. Martin, P. Savitsky, B. Diez-Dacal, M. Philpott, C. Bountra, H. Lingard, O. Fedorov, S. Muller, P.E. Brennan, S. Knapp and P. Flippakopoulos (2013). “RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.” Prox Natl Acad Sci U.S.A. 110(49): 19754-19759 (Abstract)(Abstract)

McLure K.G., E.M. Gesner, L. Tsujikawa, O.A. Kharenko, S. Attwell, E. Campeau. S. Wasiak, A. Stein, A. White, E. Fontano, R.K. Suto, N.C. Wong, G.S. Wagner, H.C. Hansen and P.R. Young (2013). “RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist.” PLoS One 8(12): e83190 (Abstract)(Abstract)

Bailey D., R. Jahagirdar, A. Gordon, A. Hafiane, S. Campbell, S. Chatur, G.S. Wagner, H.C. Hansen, F.S. Chiacchia, J. Johansson, L. Krimbou, N.C. Wong, J. Genest (2010). “RVX-208: A small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo.” J Am Coll Cardiol 55(23): 2580-2589 (Abstract)(Abstract)

Nicholls, S.J., A. Gordon, J. Johannson, C.M. Ballantyne, P.J. Barter, H.B. Brewer, J.J. Kasterlein, N.C. Wong, M.R. Borgman, S.E. Nissen (2012). “ApoA-I induction as a potential cardioprotective strategy: Rationale for the SUSTAIN and ASSURE studies.” Cardiovasc Drugs Ther 26(2): 181-187 (Abstract)(Abstract)

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Product Details

Additional Information

Quantities Please contact us for larger or different quantities
Catalog ASIS-P044
Formal Name 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one
CAS Number RVX-208 is a potent BET bromodomain inhibitor
Molecular Weight 370.399078369141
Formula C20 H22 N2 O5
Lead Time 3
LogP No
Purity 95
SMILES C12C(=O)NC(C3=CC(C)=C(OCCO)C(C)=C3)=NC1=CC(OC)=CC=2OC
Solubility and Handling No
inchikey NETXMUIMUZJUTB-UHFFFAOYSA-N
TPSA No
HBD No
HBA No
References

Details

Picaud, S., C. Wells, I. Felletar, D. Brotherton, S. Martin, P. Savitsky, B. Diez-Dacal, M. Philpott, C. Bountra, H. Lingard, O. Fedorov, S. Muller, P.E. Brennan, S. Knapp and P. Flippakopoulos (2013). “RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.” Prox Natl Acad Sci U.S.A. 110(49): 19754-19759 (Abstract)(Abstract)

McLure K.G., E.M. Gesner, L. Tsujikawa, O.A. Kharenko, S. Attwell, E. Campeau. S. Wasiak, A. Stein, A. White, E. Fontano, R.K. Suto, N.C. Wong, G.S. Wagner, H.C. Hansen and P.R. Young (2013). “RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist.” PLoS One 8(12): e83190 (Abstract)(Abstract)

Bailey D., R. Jahagirdar, A. Gordon, A. Hafiane, S. Campbell, S. Chatur, G.S. Wagner, H.C. Hansen, F.S. Chiacchia, J. Johansson, L. Krimbou, N.C. Wong, J. Genest (2010). “RVX-208: A small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo.” J Am Coll Cardiol 55(23): 2580-2589 (Abstract)(Abstract)

Nicholls, S.J., A. Gordon, J. Johannson, C.M. Ballantyne, P.J. Barter, H.B. Brewer, J.J. Kasterlein, N.C. Wong, M.R. Borgman, S.E. Nissen (2012). “ApoA-I induction as a potential cardioprotective strategy: Rationale for the SUSTAIN and ASSURE studies.” Cardiovasc Drugs Ther 26(2): 181-187 (Abstract)(Abstract)

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