CGI-1746
作者：齊岳
發(fā)布時(shí)間：2023-08-23
09:17:17
點(diǎn)擊數(shù)：
產(chǎn)品名稱：CGI-1746
產(chǎn)品描述：
| 產(chǎn)品描述 | CGI1746 is a potent and highly selective small-molecule Btk inhibitor with IC50 of 1.9 nM. |
| 靶點(diǎn)活性 | BTK:1.9 nM |
| 體外活性 | CGI1746治療（100 mg/kg,s.c,每日兩次給藥）導(dǎo)致整體臨床關(guān)節(jié)炎的顯著抑制（97％）.在陽(yáng)性抗膠原蛋白II抗體誘導(dǎo)的關(guān)節(jié)炎模型中,CGI1746處理顯著降低TNFα,IL-1β和IL-6以及MCP1和MIP-1αmRNA和蛋白質(zhì)水平.CGI1746在患有關(guān)節(jié)炎的小鼠和大鼠體內(nèi),CGI1746顯示與TNFα阻斷較好的效力,并明顯降低其臨床評(píng)分,同時(shí)減少關(guān)節(jié)炎癥. |
| 體內(nèi)活性 | CGI1746有效抑制從四個(gè)捐贈(zèng)人的扁桃體中分離出的CD27+IgG+ B細(xì)胞的增殖,平均IC50為112 nM。CGI1746完全抑制抗IgM誘導(dǎo)的小鼠和人B細(xì)胞增殖,IC50s分別為134 nM 和 42 nM,但對(duì)抗CD3和抗CD28誘導(dǎo)的T細(xì)胞增殖沒有影響。CGI1746在巨噬細(xì)胞中,消除FcγRIII誘導(dǎo)的TNFα,IL-1β和IL-6產(chǎn)生。CGI1746有效抑制固定化或可溶性的免疫復(fù)合物刺激的人單核細(xì)胞中TNFα和 IL-1β的產(chǎn)生,并較小程度地抑制IL-6產(chǎn)生。CGI1746對(duì)Btk具有特異性,選擇性比Tec和Src家族激酶高～1,000倍。 |
| 細(xì)胞實(shí)驗(yàn) | 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. |
| 分子量 | 579.701 |
| 分子式 | C34H37N5O4 |
| CAS No. | 910232-84-7 |
存儲(chǔ)
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: <1 mg/mL
DMSO: 95 mg/mL (163.9 mM)
Ethanol: 33 mg/mL (57 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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