GSK2983559
目录号 : GC36189
A RIPK2 inhibitor
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
GSK2983559 is a receptor-interacting protein kinase 2 (RIPK2) inhibitor.1 It inhibits RIPK2 by 65% in a kinase assay when used at a concentration of 10 ?M. GSK2983559 (10 ?M) also inhibits VEGFR3 by greater than 90%, as well as 14 additional kinases by 60 to 89% in a panel of 344 kinases. In vivo, GSK2983559 (7.5 and 145 mg/kg twice per day) reduces colonic damage in a mouse model of TNBS-induced colitis. GSK2983559 is also a prodrug that is cleaved to an active metabolite in the gastrointestinal tract that inhibits RIPK2 more potently than GSK2983559.
1.Haile, P.A., Casillas, L.N., Votta, B.J., et al.Discovery of a first-in-class receptor interacting protein 2 (RIP2) kinase specific clinical candidate, 2-((4-(benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl dihydrogen phosphate, for the treatment of inflammatory diseasesJ. Med. Chem.62(14)6482-6494(2019)
| Cas No. | SDF | ||
| Canonical SMILES | CC(C)(C)S(C(C(OCCOP(O)([O-])=O)=CC1=NC=N2)=CC1=C2NC3=CC(N=CS4)=C4C=C3)(=O)=O.[H]O[H].[H]O[H].[H]O[H].[Ca+2].[1/2] | ||
| 分子式 | C21H28CaN4O10PS2 | 分子量 | 611.61 |
| 溶解度 | DMF: slightly soluble,DMSO: 1 mg/ml,PBS (pH 7.2): 1 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 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℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.635 mL | 8.1751 mL | 16.3503 mL |
| 5 mM | 0.327 mL | 1.635 mL | 3.2701 mL |
| 10 mM | 0.1635 mL | 0.8175 mL | 1.635 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Publisher Correction: Death by inflammation: drug makers chase the master controller
Nat Biotechnol 2019 Apr;37(4):480.PMID:30842600DOI:10.1038/s41587-019-0082-6
In the version of this article initially published, a GlaxoSmithKline compound referred to as GSK298559 was listed in Table 1 as a RIPK1 inhibitor in phase 1 trials for inflammatory bowel disease. The correct designation is GSK2983559; however, this compound is a RIPK2 inhibitor and thus should not have been included in the table in question. The table row has been deleted. The error has been corrected in the HTML and PDF versions of the article.