INCB057643
Catalog No.S8714
Molecular Weight(MW): 415.46
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 the BET proteins and acetylated lysines on histones.
Purity & Quality Control
Choose Selective Epigenetic Reader Domain Inhibitors
Biological Activity
| Description | 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 the BET proteins and acetylated lysines on histones. | |
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| Targets |
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| 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 INCB057643 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 INCB057643. 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]. INCB057643 inhibits proliferation of prostate cancer cell lines. In short-term cell proliferation assays, INCB057643 appears more effective against androgen-dependent (VCaP and LNCaP) than androgen-independent (DU145 and PC3) cells[2]. |
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| 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 INCB057643 (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]. |
Protocol
Solubility (25°C)
| In vitro | DMSO | 83 mg/mL (199.77 mM) |
|---|---|---|
| Water | Insoluble | |
| Ethanol | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 415.46 |
|---|---|
| Formula | C20H21N3O5S |
| CAS No. | 1820889-23-3 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
Bio Calculators
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Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02959437 | Active not recruiting | Solid Tumors|Advanced Malignancies|Metastatic Cancer | Incyte Corporation | January 26 2017 | Phase 1|Phase 2 |
| NCT02959437 | Active not recruiting | Solid Tumors|Advanced Malignancies|Metastatic Cancer | Incyte Corporation | January 26 2017 | Phase 1|Phase 2 |
| NCT02711137 | Active not recruiting | Solid Tumors | Incyte Corporation | May 2016 | Phase 1|Phase 2 |
| NCT02711137 | Active not recruiting | Solid Tumors | Incyte Corporation | May 2016 | Phase 1|Phase 2 |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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