1820889-23-3
1820889-23-3 structure
- Name: INCB-057643
- Chemical Name: INCB-057643
- CAS Number: 1820889-23-3
- Molecular Formula: C20H21N3O5S
- Molecular Weight: 415.46
- Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
- Create Date: 2018-03-09 13:54:37
- Modify Date: 2024-01-10 12:21:42
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INCB-057643 is a novel, orally bioavailable BET inhibitor.
| Name | INCB-057643 |
|---|
| 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 |
| Molecular Formula | C20H21N3O5S |
|---|---|
| Molecular Weight | 415.46 |
| Storage condition | 2-8℃ |