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INCB-057643

Catalog No. T5417   CAS 1820889-23-3

INCB057643 is a potent, selective and orally bioavailable BET inhibitor.

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INCB-057643 Chemical Structure
INCB-057643, CAS 1820889-23-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 68.00
2 mg In stock $ 98.00
5 mg In stock $ 169.00
10 mg In stock $ 289.00
25 mg In stock $ 548.00
50 mg In stock $ 779.00
100 mg In stock $ 1,060.00
500 mg In stock $ 2,130.00
1 mL * 10 mM (in DMSO) In stock $ 183.00
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Purity: 99.58%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description INCB057643 is a potent, selective and orally bioavailable BET inhibitor.
In vitro INCB057643 inhibited binding of BRD2/BRD3/BRD4 to an acetylated histone H4 peptide in the low nM range and was selective against other bromodomain-containing proteins. INCB057643 inhibited proliferation of human AML, DLBCL, and multiple myeloma cell lines, with a corresponding decrease in MYC protein levels. Cell cycle analyses indicated that G1 arrest and a concentration-dependent increase in apoptosis were seen within 48 hours of treatment with INCB057643. BRD proteins also regulate the expression of many pro-inflammatory genes. Production of several cytokines, including IL-6, IL-10 and MIP-1α, was repressed by INCB057643 in human and mouse whole blood stimulated ex vivo with LPS [1].
In vivo Oral administration of INCB057643 resulted in significant anti-tumor efficacy in xenograft models of AML, myeloma, and DLBCL. Additionally, combining INCB057643 with the standard of care agents used for the treatment of DLBCL including rituximab and bendamustine resulted in enhanced anti-tumor efficacy relative to that achieved with single-agent therapies at doses that were well tolerated [1].
Molecular Weight 415.46
Formula C20H21N3O5S
CAS No. 1820889-23-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/mL (144.42 mM)

TargetMolReferences and Literature

1. Matthew C. Stubbs, et al. Abstract 5071: Preclinical characterization of the potent and selective BET inhibitor INCB057643 in models of hematologic malignancies. AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 5071. 2. Wilson AJ, et al. The BET inhibitor INCB054329 reduces homologous recombination efficiency and augments PARP inhibitor activity in ovarian cancer. Gynecol Oncol. 2018 Jun;149(3):575-584.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Histone Modification Compound Library Apoptosis Compound Library PPI Inhibitor Library Inhibitor Library Anti-Cancer Compound Library Clinical Compound Library Drug Repurposing Compound Library

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Keywords

INCB-057643 1820889-23-3 Apoptosis Chromatin/Epigenetic Epigenetic Reader Domain inhibit Inhibitor INCB057643 INCB 057643 inhibitor

 

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