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CGI-1746

目录号: PL02420 纯度: ≥98%

CGI-1746 是一种有效的，高选择性的 Btk 抑制剂，IC50 值为 1.9 nM。

CAS No. :910232-84-7

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中文名称	CGI-1746
中文别名	N-[3-[4,5-二氢-4-甲基-6-[[4-(4-吗啉基羰基)苯基]氨基]-5-氧代-2-吡嗪基]-2-甲基苯基]-4-(叔丁基)苯甲酰胺;CGI-1746 抑制剂
英文名称	CGI-1746
英文别名	N-[3-[4,5-Dihydro-4-methyl-6-[[4-(4-morpholinylcarbonyl)phenyl]amino]-5-oxo-2-pyrazinyl]-2-methylphenyl]-4-(tert-butyl)benzamide;CGI-1746;4-tert-butyl-N-[2-methyl-3-[4-methyl-6-[4-(morpholine-4-carbonyl)anilino]-5-oxopyrazin-2-yl]phenyl]benzamide;C34H37N5O4;Cgi 1746;4-tert-butyl-N-(2-methyl-3-{4-methyl-6-[4-(morpholine-4-carbonyl)-phenylamino]-5-oxo-4,5-dihydro-pyrazin-2-yl}-phenyl)-benzamide;CGI1746,2;CS-0252;CGI1746;4-(tert-Butyl)-N-(2-methyl-3-(4-methyl-6-((4-(morpholine-4-carbonyl)phenyl)amino)-5-oxo-4,5-dihydropyrazin-2-yl)phenyl)benzamide;GCI1746;4-Tert-Butyl-N-[2-Methyl-3-(4-Methyl-6-{[4-(Morpholin-4-Ylcarbonyl)phenyl]amino}-5-Oxo-4,5-Dihydropyrazin-2-Yl)phenyl]benzamide;GTPL8066;BDBM36516;SYN1164;Benzamide, N-[3-[4,5-dihydro-4-methyl-6-[[4-(4-morpholinylcarbonyl)phenyl]amino]-5-oxopyrazinyl]-2-methylphenyl]-4-(1,1-dimethylethyl)- (9CI);N-[3-[4,5-Dihydro-4-methyl-6-[[4-(4-morpholinylcarbonyl)phenyl]amino]-5-oxo-2-pyrazinyl]-2-methylphenyl]-4-(1,1-dimethylethyl)benzamide (ACI);CGI 1746
Cas No.	910232-84-7
分子式	C₃₄H₃₇N₅O₄
分子量	579.69
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	CGI-1746 是一种有效的，高选择性的 Btk 抑制剂，IC50 值为 1.9 nM。

产品详情	CGI-1746 是一种有效的，高选择性的 Btk 抑制剂，IC₅₀ 值为 1.9 nM。
生物活性	CGI-1746 is a potent and highly selective inhibitor of the Btk with IC 50 of 1.9 nM.
性状	Solid
IC50 & Target[1][2]	IC50: 1.9 nM (Btk)
体外研究(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,
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Di Paolo, Julie A. et al. Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis. Nature Chemical Biology (2011), 7(1), 41-50 [2]. Kokabee L, et al. Brutons tyrosine kinase is a potential therapeutic target in prostate cancer. Cancer Biol Ther. 2015;16(11):1604-15

溶解度数据	In Vitro: DMSO : ≥ 50 mg/mL (86.25 mM)配制储备液

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[1]. Di Paolo, Julie A. et al. Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis. Nature Chemical Biology (2011), 7(1), 41-50
[2]. Kokabee L, et al. Brutons tyrosine kinase is a potential therapeutic target in prostate cancer. Cancer Biol Ther. 2015;16(11):1604-15

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

CGI-1746

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