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Compound 7 (Fedorov, 2014), a [1,2,4]triazolo[4,3-a]phthalazine bromodomain inhibitor

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Catalog: ASIS-P004

Formal Name: Compound 7 (Fedorov, 2014), a [1,2,4]triazolo[4,3-a]phthalazine bromodomain inhibitor

Produced By: AsisChem, Inc.

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pdfASIS-P004 Technical Product Information (563.95 KB )

Biological Description

ASIS-P004, published as Compound 7 (Fedorov, 2014), is a [1,2,4]triazolo[4,3-a]phthalazine bromodomain inhibitor with high potency (DSF ?Tm? of 1-3) against BRD9 as well as moderate activity (DSF ?Tm? of 1-3) against CECR2, BRD4(1), BRD4(2), and CREBBP. Histone modification plays a vital role in epigenetic regulation and is increasingly being studied as a mechanism and potential drug target for a variety of diseases including some carcinomas, leukemia, various inflammatory diseases and HIV. Lysine acetylation of histones is mediated by proteins containing a bromodomain, an approximately 110 amino acid conserved domain. Many of these bromodomain proteins, including BRD3, BRD4, CREBBP, TIF1?, ATAD2, and SMARCA4 are studied for their roles in disease and pathology.

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Additional Information

Quantities Please contact us for larger or different quantities
Catalog ASIS-P004
Formal Name Compound 7 (Fedorov, 2014), a [1,2,4]triazolo[4,3-a]phthalazine bromodomain inhibitor
CAS Number -
Molecular Weight 367.424896240234
Formula C18 H17 N5 O2 S
Lead Time 3
LogP No
Purity 95
SMILES C1(=NN2C(C)=NN=C2C2C=CC=CC1=2)C1C=C(S(=O)(=O)NC)C(C)=CC=1
Solubility and Handling No
inchikey ABQMPFKFBYVSKA-UHFFFAOYSA-N
TPSA No
HBD No
HBA No

Details

Bamborough, P., H. Diallo, J. D. Goodacre, L. Gordon, A. Lewis, J. T. Seal, D. M. Wilson, M. D. Woodrow and C. W. Chung (2012). "Bamborough, P part 2: optimization of phenylisoxazole sulfonamides." J Med Chem 55(2): 587-596. (Abstract) (Abstract)

Demont, E. H., C. W. Chung, R. C. Furze, P. Grandi, A. M. Michon, C. Wellaway, N. Barrett, A. M. Bridges, P. D. Craggs, H. Diallo, D. P. Dixon, C. Douault, A. J. Emmons, E. J. Jones, B. V. Karamshi, K. Locke, D. J. Mitchell, B. H. Mouzon, R. K. Prinjha, A. D. Roberts, R. J. Sheppard, R. J. Watson and P. Bamborough (2015). "Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors." J Med Chem 58(14): 5649-5673. (Abstract) (Abstract)

Fedorov, O., H. Lingard, C. Wells, O. P. Monteiro, S. Picaud, T. Keates, C. Yapp, M. Philpott, S. J. Martin, I. Felletar, B. D. Marsden, P. Filippakopoulos, S. Muller, S. Knapp and P. E. Brennan (2014). "[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains." J Med Chem 57(2): 462-4763906316. (Abstract) (Abstract)

Zhao, H., L. Gartenmann, J. Dong, D. Spiliotopoulos and A. Caflisch (2014). "Discovery of BRD4 bromodomain inhibitors by fragment-based high-throughput docking." Bioorg Med Chem Lett 24(11): 2493-2496. (Abstract) (Abstract)

Zhao, L., D. Cao, T. Chen, Y. Wang, Z. Miao, Y. Xu, W. Chen, X. Wang, Y. Li, Z. Du, B. Xiong, J. Li, C. Xu, N. Zhang, J. He and J. Shen (2013). "Fragment-based drug discovery of 2-thiazolidinones as inhibitors of the histone reader BRD4 bromodomain." J Med Chem 56(10): 3833-3851. (Abstract) (Abstract)

Zhao, L., Y. Wang, D. Cao, T. Chen, Q. Wang, Y. Li, Y. Xu, N. Zhang, X. Wang, D. Chen, L. Chen, Y. L. Chen, G. Xia, Z. Shi, Y. C. Liu, Y. Lin, Z. Miao, J. Shen and B. Xiong (2015). "Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization." J Med Chem 58(3): 1281-1297. (Abstract) (Abstract)

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Product Details

Additional Information

Quantities Please contact us for larger or different quantities
Catalog ASIS-P004
Formal Name Compound 7 (Fedorov, 2014), a [1,2,4]triazolo[4,3-a]phthalazine bromodomain inhibitor
CAS Number -
Molecular Weight 367.424896240234
Formula C18 H17 N5 O2 S
Lead Time 3
LogP No
Purity 95
SMILES C1(=NN2C(C)=NN=C2C2C=CC=CC1=2)C1C=C(S(=O)(=O)NC)C(C)=CC=1
Solubility and Handling No
inchikey ABQMPFKFBYVSKA-UHFFFAOYSA-N
TPSA No
HBD No
HBA No
References

Details

Bamborough, P., H. Diallo, J. D. Goodacre, L. Gordon, A. Lewis, J. T. Seal, D. M. Wilson, M. D. Woodrow and C. W. Chung (2012). "Bamborough, P part 2: optimization of phenylisoxazole sulfonamides." J Med Chem 55(2): 587-596. (Abstract) (Abstract)

Demont, E. H., C. W. Chung, R. C. Furze, P. Grandi, A. M. Michon, C. Wellaway, N. Barrett, A. M. Bridges, P. D. Craggs, H. Diallo, D. P. Dixon, C. Douault, A. J. Emmons, E. J. Jones, B. V. Karamshi, K. Locke, D. J. Mitchell, B. H. Mouzon, R. K. Prinjha, A. D. Roberts, R. J. Sheppard, R. J. Watson and P. Bamborough (2015). "Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors." J Med Chem 58(14): 5649-5673. (Abstract) (Abstract)

Fedorov, O., H. Lingard, C. Wells, O. P. Monteiro, S. Picaud, T. Keates, C. Yapp, M. Philpott, S. J. Martin, I. Felletar, B. D. Marsden, P. Filippakopoulos, S. Muller, S. Knapp and P. E. Brennan (2014). "[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains." J Med Chem 57(2): 462-4763906316. (Abstract) (Abstract)

Zhao, H., L. Gartenmann, J. Dong, D. Spiliotopoulos and A. Caflisch (2014). "Discovery of BRD4 bromodomain inhibitors by fragment-based high-throughput docking." Bioorg Med Chem Lett 24(11): 2493-2496. (Abstract) (Abstract)

Zhao, L., D. Cao, T. Chen, Y. Wang, Z. Miao, Y. Xu, W. Chen, X. Wang, Y. Li, Z. Du, B. Xiong, J. Li, C. Xu, N. Zhang, J. He and J. Shen (2013). "Fragment-based drug discovery of 2-thiazolidinones as inhibitors of the histone reader BRD4 bromodomain." J Med Chem 56(10): 3833-3851. (Abstract) (Abstract)

Zhao, L., Y. Wang, D. Cao, T. Chen, Q. Wang, Y. Li, Y. Xu, N. Zhang, X. Wang, D. Chen, L. Chen, Y. L. Chen, G. Xia, Z. Shi, Y. C. Liu, Y. Lin, Z. Miao, J. Shen and B. Xiong (2015). "Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization." J Med Chem 58(3): 1281-1297. (Abstract) (Abstract)

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