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CGI-1746

SKU: orb1305433

Description

CGI1746 is a potent and highly selective small-molecule inhibitor of Bruton's tyrosine kinase (Btk), exhibiting an IC50 of 1.9 nM. It is a valuable research tool for investigating Btk-related signaling in immunological and oncological research, applicable in both in vitro biochemical assays and in vivo disease models.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Images & Validation

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CGI-1746

Key Properties

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CAS Number910232-84-7
MW579.69
Purity98.27%
FormulaC34H37N5O4
SMILESCC1=C(C=CC=C1NC(=O)C2=CC=C(C(C)(C)C)C=C2)C=3N=C(NC4=CC=C(C(=O)N5CCOCC5)C=C4)C(=O)N(C)C3
TargetAutophagy,BTK
SolubilityH2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:33 mg/mL (56.93 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (5.69 mM);DMSO:95 mg/mL (163.88 mM)

Bioactivity

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Target IC50
BTK:1.9 nM
In Vivo
CGI1746 effectively inhibits the proliferation of CD27+IgG+ B cells isolated from the tonsils of four donors, with an average IC50 of 112 nM. It completely suppresses B cell proliferation induced by anti-IgM in both mice and humans, with IC50s of 134 nM and 42 nM, respectively, yet does not affect T cell proliferation induced by anti-CD3 and anti-CD28. In macrophages, CGI1746 eliminates the production of TNFα, IL-1β, and IL-6 triggered by FcγRIII. It also efficiently inhibits the production of TNFα and IL-1β in human monocytes stimulated by immobilized or soluble immune complexes, and to a lesser extent, reduces IL-6 production. CGI1746 shows high specificity and selectivity for Btk, being ~1,000 times more selective than for Tec and Src family kinases.
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In Vitro
Treatment with CGI1746 at a dose of 100 mg/kg, administered subcutaneously twice daily, resulted in a significant suppression (97%) of overall clinical arthritis symptoms. In a positive anti-collagen type II antibody-induced arthritis model, CGI1746 significantly reduced levels of TNFα, IL-1β, and IL-6, as well as MCP-1 and MIP-1α mRNA and protein. In mice and rats with arthritis, CGI1746 demonstrated superior efficacy compared to TNFα blockade, significantly lowering clinical scores while also reducing joint inflammation.
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Cell Research
CGI-1746 is dissolved in DMSO. 5×103 DU145 cells or 104 LNCaP cells per well, grown on 96 well plates for 24h, are treated with 1 to 30 μM BTK inhibitors. Cells are fixed after 72h with 2.5% formaldehyde, and stained with Hoechst 33342. Control cells are treated with DMSO. Cell images are acquired using an IN Cell Analyzer 2200 high content imaging system, with a 20X objective. At least 9 fields are imaged per single well of each experiment. Cell numbers are determined and statistics performed using IN Cell Investigator 3.4 high content image analysis software. Each experiment is replicated 3 times, and data are presented as mean±SD. Results are considered significant if p < 0.05.
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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inhibit, Inhibitor, Autophagy, Btk, BTK, Bruton tyrosine kinase, CGI1746, CGI-1746, CGI 1746

Similar Products

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  • CGI-1746

    CGI-1746 [orb1223679]

    >98% (HPLC)

    910232-84-7

    579.6887

    C34H37N5O4

    5 mg, 10 mg, 50 mg, 2 mg, 100 mg, 1 g, 500 mg, 200 mg, 25 mg
Quality Guarantee

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Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Compound Identifiers

PubChem CID
24857323 ↗

Key Properties

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No computed properties available.

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CGI-1746 (orb1305433)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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2 mg
$ 80.00
5 mg
$ 100.00
1 ml x 10 mM (in DMSO)
$ 120.00
10 mg
$ 130.00
25 mg
$ 160.00
50 mg
$ 200.00
100 mg
$ 280.00
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