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Postion:Product Catalog >INCB-057643
INCB-057643
  • INCB-057643

INCB-057643 NEW

Price $35 $83 $143
Package 1mg 5mg 10mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: INCB-057643 CAS No.: 1820889-23-3
Purity: 99.50% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameINCB-057643
DescriptionINCB057643 is a potent, selective and orally bioavailable BET inhibitor.
In vitroINCB057643 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 vivoOral 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].
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationDMSO : 65 mg/mL (156.45 mM), Sonication is recommended.
KeywordsApoptosis | Epigenetic Reader Domain | inhibit | Inhibitor | INCB057643 | INCB-057643 | INCB 057643
Inhibitors RelatedStavudine | 5-Fluorouracil | Acetylcysteine | Kaempferol | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Curcumin
Related Compound LibrariesHistone Modification Compound Library | Bioactive Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Orally Active Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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