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CGI1746 910232-84-7

Product Description

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Molecular Weight:

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


Biological Activity


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.


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.


Protocol(Only for Reference)


Kinase Assay: [1]

Lanthascreen assay Lanthascreen assay is performed at Km for ATP (10 μM) with human full-length Btk (C-terminal V5-His6 expressed in Sf9 cells) and quantified on an EnVision.


Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)


Species Baboon Dog Monkey Rabbit Guinea pig Rat Hamster Mouse
Weight (kg) 12 10 3 1.8 0.4 0.15 0.08 0.02
Body Surface Area (m2) 0.6 0.5 0.24 0.15 0.05 0.025 0.02 0.007
Km factor 20 20 12 12 8 6 5 3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by Animal B Km
Animal A Km



For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × mouse Km(3) = 11.2 mg/kg
rat Km(6)










Chemical Information




Molecular Weight (MW) 579.69
Formula

C34H37N5O4

CAS No. 910232-84-7

Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms N/A



Solubility (25°C) * In vitro DMSO 100 mg/mL (172.5 mM)
Water <1 mg/mL (
Ethanol 100 mg/mL (172.5 mM)
* <1 mg/ml means slightly soluble or 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 Name N-[3-[4,5-dihydro-4-methyl-6-[[4-(4-morpholinylcarbonyl)phenyl]amino]-5-oxopyrazinyl]-2-methylphenyl]-4-(1,1-dimethylethyl)-benzamide







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