ZEN-2759
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 407929

CAS#: 1616400-50-0

Description: ZEN-2759 is BRD4(BD1) inhibitor.

Chemical Structure

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ZEN-2759
CAS# 1616400-50-0
Instruction

Theoretical Analysis

MedKoo Cat#: 407929
Name: ZEN-2759
CAS#: 1616400-50-0
Chemical Formula: C17H16N2O2
Exact Mass: 280.12
Molecular Weight: 280.327
Elemental Analysis: C, 72.84; H, 5.75; N, 9.99; O, 11.41

Price and Availability

Size Price Availability Quantity
25mg USD 450 2 Weeks
50mg USD 750 2 Weeks
100mg USD 1250 2 Weeks
200mg USD 2050 2 Weeks
500mg USD 2950 2 Weeks
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Synonym: ZEN-2759; ZEN 2759; ZEN2759;

IUPAC/Chemical Name: 1-benzyl-5-(3,5-dimethylisoxazol-4-yl)pyridin-2(1H)-one

InChi Key: CIJOVPIWGFQZFF-UHFFFAOYSA-N

InChi Code: InChI=1S/C17H16N2O2/c1-12-17(13(2)21-18-12)15-8-9-16(20)19(11-15)10-14-6-4-3-5-7-14/h3-9,11H,10H2,1-2H3

SMILES Code: O=C(C=CC(C1=C(C)ON=C1C)=C2)N2CC3=CC=CC=C3

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.03.00

More Info: BET proteins are key epigenetic regulators that regulate transcription through binding to acetylated lysine (AcLys) residues of histones and transcription factors through bromodomains (BDs). The disruption of this interaction with small molecule bromodomain inhibitors is a promising approach to treat various diseases including cancer, autoimmune and cardiovascular diseases. Covalent inhibitors can potentially offer a more durable target inhibition leading to improved in vivo pharmacology.

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 280.33 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine
Olesya A. Kharenko, Reena G. Patel, S. David Brown, Cyrus Calosing, Andre White, Damodharan Lakshminarasimhan, Robert K. Suto, Bryan C. Duffy, Douglas B. Kitchen, Kevin G. McLure, Henrik C. Hansen, Edward H. van der Horst, and Peter R. Young
Publication Date (Web): August 30, 2018 (Article)
DOI: 10.1021/acs.jmedchem.8b00666