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CAS No. : 910232-84-7
MCE 国际站：CGI-1746
产品活性：CGI-1746 是一种有效的，高选择性的 Btk 抑制剂，IC50 值为 1.9 nM。
研究领域：Protein Tyrosine Kinase/RTK | Autophagy
In Vitro: CGI1746 is specific for Btk, with appr 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 has 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. CGI-1746 does not kill cells as well as the irreversible BTK inhibitors at the same drug concentration. CGI-1746 significantly reduces phosphorylation of both the BTK-A and BTK-C proteins, indicating the auto-phosphorylation of the BTK-C isoform is inhibited in a manner similar to BTK-A. CGI-1746 does not kill LNCaP or DU145 prostate cancer cells at the same concentrations as Ibrutinib or AVL-292, but it demonstrates similar inhibition of BTK phosphorylation at tyrosine 233 in the SH3 domain.
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.
相关产品：Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Autophagy Compound Library | Pyroptosis Compound Library | Chemical Probe Library | Anti-Blood Cancer Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | Highly Selective Activators Library | Atuzabrutinib | PCI 29732 | JAK3/BTK-IN-6 | Pirtobrutinib | CNX-500 | BTK inhibitor 17 | Remibrutinib | RN486 | GDC-0834 Racemate | Spebrutinib besylate | BTK inhibitor 19 | BMX-IN-1 | BMS-935177 | Ibrutinib | PF-06250112 | QL-X-138 | SJF620 hydrochloride | PROTAC BTK Degrader-2 | BTK-IN-8 | JAK3/BTK-IN-3 | JS25 | JAK3/BTK-IN-2 | (R)-Zanubrutinib | Edralbrutinib | Branebrutinib | Poseltinib | BTK inhibitor 20 | RET-IN-14 | QL47 | BTK-IN-23
热门产品线：重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
Trending products：Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
货号: HY-11999
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