Home Epigenetics Epigenetic Reader Domain inhibitor INCB057643

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INCB057643 Epigenetic Reader Domain inhibitor

Cat.No.S8714

INCB057643 is a BET inhibitor that binds to the acetylated lysine recognition motifs found in the BRD of BET proteins, thereby preventing the interaction between this compound and acetylated lysines on histones.
INCB057643 Epigenetic Reader Domain inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 415.46

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Quality Control

Chemical Information, Storage & Stability

Molecular Weight 415.46 Formula

C20H21N3O5S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1820889-23-3 -- Storage of Stock Solutions

Synonyms N/A Smiles CC1(C(=O)N(C2=CC(=CC(=C2O1)C3=CN(C(=O)C4=C3C=CN4)C)S(=O)(=O)C)C)C

Solubility

In vitro
Batch:

DMSO : 83 mg/mL (199.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
BET [2]
In vitro

INCB057643 inhibits binding of BRD2/BRD3/BRD4 to an acetylated histone H4 peptide in the low nM range, and is selective against other bromodomain containing proteins. In vitro analyses show that this compound inhibits proliferation of human AML, DLBCL, and multiple myeloma cell lines, with a corresponding decrease in MYC protein levels. Cell cycle analyses indicate that G1 arrest and a concentration-dependent increase in apoptosis are seen within 48 hours of treatment with this chemical. Production of several cytokines, including IL-6, IL-10 and MIP-1α, was repressed by this compound in human and mouse whole blood stimulated ex vivo with LPS[1]. It inhibits proliferation of prostate cancer cell lines. In short-term cell proliferation assays, this chemical appears more effective against androgen-dependent (VCaP and LNCaP) than androgen-independent (DU145 and PC3) cells[2].
In vivo

Oral administration of INCB057643 resulted in significant anti-tumor efficacy in xenograft models of AML, myeloma, and DLBCL[1]. Treatment of mice bearing 22Rv1 tumor xenografts with this compound (3 mg/kg) led to significant inhibition of tumor growth (T/C%:45%) and consistent reduction of tumor weight relative to vehicle-treated mice[2].
References

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