CGI-1746 is a selective and potent inhibitor of Bruton's tyrosine kinase (BTK) with IC50 value of 1.9 nM [1][2].
Bruton's tyrosine kinase (BTK) is a member of the Tec tyrosine kinase family and plays an important role in differentiation, proliferation and development of B cells. It is an attractive target for the treatment of immunological disorders such as B-cell malignancies, rheumatoid arthritis (RA), multiple sclerosis (MS) and lupus [3].
CGI-1746 potently inhibits both auto- and transphosphorylation of BTK. It binds to un-phosphorylated BTK and stabilizes it in an inactive enzyme state. In cellular assays, CGI-1746 blocks BCR-mediated B-cell proliferation and suppresses the production of IL-6, IL-1βand TNF in macrophages [1].
In experimental mouse models, CGI-1746 shows a robust anti-arthritic activity [1]. In B10.RIII mice model, CGI1746 resulted in a significant inhibition (97%) of clinical arthritis scores, which were better than dexamethasone treatment (56% inhibition) [2].
References:
[1]. Akinleye A, Chen Y, Mukhi N, et al. Ibrutinib and novel BTK inhibitors in clinical development. J Hematol Oncol, 2013, 6: 59.
[2]. Di Paolo JA, Huang T, Balazs M, et al. Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis. Nat Chem Biol, 2011, 7(1): 41-50.
[3]. Young WB, Barbosa J, Blomgren P, et al. Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834. Bioorg Med Chem Lett, 2015, 25(6): 1333-1337.
CGI-1746
| 规格 | 价格 | 库存 | 数量 | 操作 |
|---|---|---|---|---|
| 1mg | ¥382.00 | 现货 | 1 | |
| 5mg | ¥891.00 | 现货 | 1 | |
| 10mg | ¥1,395.00 | 现货 | 1 | |
| 25mg | ¥2,453.00 | 现货 | 1 | |
| 50mg | ¥3,780.00 | 现货 | 1 | |
| 100mg | ¥5,310.00 | 现货 | 1 | |
| 10mM (in 1mL DMSO) | ¥1,137.00 | 现货 | 1 |
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产品描述 Description
实验参考方法 Experimental Reference Method
| Cell experiment [1]: | |
|
Cell lines |
Human B cells |
|
Preparation method |
The solubility of this compound in DMSO is > 29 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
|
Reacting condition |
0.003 ~ 10 μM |
|
Applications |
In human B cells, CGI-1746 potently inhibited anti-IgM-induced phosphorylation of Btk Tyr223, Btk Tyr551 and PLCγ2 Tyr1217, with an average IC50 value of 2.9 nM. In addition, CGI-1746 lowered the basal phosphorylation levels of Btk Tyr551 and Tyr223, but not the basal phosphorylation of PLCγ2 Tyr1217. |
| Animal experiment [1]: | |
|
Animal models |
Collagen-induced arthritis (CIA) mouse model |
|
Dosage form |
100 mg/kg; s.c.; b.i.d., from day 12 to day 26 |
|
Applications |
CGI-1746 significantly inhibited overall clinical arthritis scores (97% inhibition). Moreover, CGI-1746 substantially reduced anti-collagen II (CII) titers. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Di Paolo JA, Huang T, Balazs M, et al. Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis. Nat Chem Biol, 2011, 7(1): 41-50. |
产品文档 Product Documents
化学性质Chemical Properties
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。