INCB-057643

Modify Date: 2024-01-10 12:21:42

INCB-057643 Structure
INCB-057643 structure
Common Name INCB-057643
CAS Number 1820889-23-3 Molecular Weight 415.46
Density N/A Boiling Point N/A
Molecular Formula C20H21N3O5S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of INCB-057643


INCB-057643 is a novel, orally bioavailable BET inhibitor.

 Names

Name INCB-057643

 INCB-057643 Biological Activity

Description INCB-057643 is a novel, orally bioavailable BET inhibitor.
Related Catalog
Target

BET[1]

In Vitro INCB-057643 is a novel, orally bioavailable BET inhibitor. INCB-057643 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 INCB-057643 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 INCB-057643[1].
In Vivo Production of several cytokines, including IL-6, IL-10 and MIP-1α, is repressed by INCB-057643 in human and mouse whole blood stimulated ex vivo with LPS. Oral administration of INCB-057643 results in significant anti-tumor efficacy in xenograft models of AML, myeloma, and DLBCL. Additionally, combining INCB-057643 with standard of care agents used for the treatment of DLBCL including rituximab and bendamustine results in enhanced anti-tumor efficacy relative to that achieved with single agent therapies at doses that are well tolerated[1].
References

[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.

 Chemical & Physical Properties

Molecular Formula C20H21N3O5S
Molecular Weight 415.46
Storage condition 2-8℃
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