For research use only.

Catalog No.S7051

6 publications

CGI1746 Chemical Structure

CAS No. 910232-84-7

CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM.

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Selleck's CGI1746 has been cited by 6 publications

2 Customer Reviews

  • Cleaved IL-1β and caspase-1 from primed and nigericin-treated human primary MoMacs pretreated with DMSO (mock), ibrutinib, or CGI-1746 for 10 minutes. Pro-IL-1β and caspase-1 processing in primary MoMacs was strongly reduced by both ibrutinib and CGI1746.

    J Allergy Clin Immunol, 2017, 140(4):1054-1067. CGI1746 purchased from Selleck.

    IL-1β cleavage (A, B) in platelets activated by collagen or thrombin is reduced in the presence of the BTK inhibitor CGI1746.

    Biochem Biophys Res Commun, 2017, 483(1):230-236. CGI1746 purchased from Selleck.

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Biological Activity

Description CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM.
BTK [1]
(Cell-free assay)
1.9 nM
In vitro

CGI1746 is specific for Btk, with ∼1,000-fold selectivity over Tec and Src family kinases. In an ATP-free competition binding assay, the dissociation constant for Btk is 1.5 nM. CGI1746 inhibits Btk activity in a new binding mode that stabilizes an inactive nonphosphorylated enzyme conformation. CGI1746 inhibits both auto- and transphosphorylation steps necessary for enzyme activation. CGI1746 completely inhibits anti-IgM–induced murine and human B cell proliferation, with IC50s of 134 nM and 42 nM, respectively, but had no effect on anti-CD3- and anti-CD28–induced T cell proliferation. CGI1746 potently inhibits the proliferation of CD27+IgG+ B cells isolated from the tonsils of four human donors with an average IC50 of 112 nM. In macrophages, CGI1746 abolishes FcγRIII-induced TNFα, IL-1β and IL-6 production. CGI1746 potently inhibits TNFα, IL-1β and, to a lesser extent, IL-6 (three- to eight-fold higher IC50) production in human monocytes stimulated with immobilized or soluble immune complexes. [1]

In vivo CGI1746 abrogates B cell–dependent arthritis. CGI1746 treatment (100 mg/kg, s.c, twice-daily dosing) results in significant inhibition (97%) of overall clinical arthritis scores. CGI1746 treatment substantially reduces TNFα, IL-1β and IL-6, as well as MCP1 and MIP-1α on both the mRNA and protein level in the passive anti-collagen II antibody–induced arthritis (CAIA) model. CGI1746 shows comparable efficacy to TNFα blockade and significantly reduces clinical scores, as well as joint inflammation, in mice or rats with established arthritis. [1]


Solubility (25°C)

In vitro DMSO 100 mg/mL (172.5 mM)
Ethanol 33 mg/mL warmed (56.92 mM)
Water 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 579.69


CAS No. 910232-84-7
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(C=CC=C1NC(=O)C2=CC=C(C=C2)C(C)(C)C)C3=CN(C(=O)C(=N3)NC4=CC=C(C=C4)C(=O)N5CCOCC5)C

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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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BTK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID