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CGI1746 BTK inhibitor

Cat.No.S7051

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

Chemical Structure

Molecular Weight: 579.69

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Quality Control

Batch: Purity: 99.86%
99.86

Solubility

In vitro
Batch:

DMSO : 250 mg/mL (431.26 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 33 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 579.69 Formula

C34H37N5O4

 Storage (From the date of receipt)
CAS No. 910232-84-7 Download SDF Storage of Stock Solutions

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

Mechanism of Action

Targets/IC50/Ki
BTK
(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. This compound inhibits Btk activity in a new binding mode that stabilizes an inactive nonphosphorylated enzyme conformation. It inhibits both auto- and transphosphorylation steps necessary for enzyme activation. This chemical 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. It 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, this compound abolishes FcγRIII-induced TNFα, IL-1β and IL-6 production. It 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.
In vivo
CGI1746 abrogates B cell–dependent arthritis. This compound treatment (100 mg/kg, s.c, twice-daily dosing) results in significant inhibition (97%) of overall clinical arthritis scores. This compound 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. This compound shows comparable efficacy to TNFα blockade and significantly reduces clinical scores, as well as joint inflammation, in mice or rats with established arthritis.
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