PRT062607 (P505-15)
(Synonyms: 2-[[(1R,2S)-2-氨基环己基]氨基]-4-[[3-(2H-1,2,3-三唑-2-基)苯基]氨基]-5-嘧啶甲酰胺,P505-15; PRT-2607; BIIB-057) 目录号 : GC31819
A potent, orally bioavailable Syk inhibitor
Cas No.:1370261-96-3
Sample solution is provided at 25 µL, 10mM.
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BIIB-057 is a potent inhibitor of the non-receptor tyrosine kinase Syk (IC50 = 1 nM).1 It displays at least 80-fold selectivity for Syk over other kinases. BIIB-057 blocks B cell receptor-mediated cell signaling and activation in whole blood (IC50s = 0.27 and 0.28 ?M, respectively), as well as Fc? receptor 1-mediated basophil degranulation (IC50 = 0.15 ?M).1 It antagonizes chemokine production, cell migration, and survival of chronic lymphocytic leukemia (CLL) cells after B cell receptor activation and synergistically enhances the action of fludarabine in killing CLL cells.2,3 BIIB-057 is orally bioavailable, as it produces dose-dependent anti-inflammatory activity in two rodent models of rheumatoid arthritis.1 It also prevents splenomegaly and inhibits non-Hodgkin lymphoma tumor growth in a xenograft model.3
1.Coffey, G., DeGuzman, F., Inagaki, M., et al.Specific inhibition of spleen tyrosine kinase suppresses leukocyte immune function and inflammation in animal models of rheumatoid arthritisJ. Pharmacol. Exp. Ther.340(2)350-359(2012) 2.Hoellenriegel, J., Coffey, G.P., Sinha, U., et al.Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migrationLeukemia26(7)1576-1583(2012) 3.Spurgeon, S.E., Coffey, G., Fletcher, L.B., et al.The selective Syk inhibitor P505-15 (PRT062607) inhibits B cell signaling and function in vitro and in vivo and augments the activity of fludarabine in chronic lymphocytic leukemiaJ. Pharmacol. Exp. Ther.344(2)378-387(2015)
| Cas No. | 1370261-96-3 | SDF | |
| 别名 | 2-[[(1R,2S)-2-氨基环己基]氨基]-4-[[3-(2H-1,2,3-三唑-2-基)苯基]氨基]-5-嘧啶甲酰胺,P505-15; PRT-2607; BIIB-057 | ||
| Canonical SMILES | NC(C1=CN=C(N[C@H]2[C@@H](N)CCCC2)N=C1NC3=CC=CC(N4N=CC=N4)=C3)=O | ||
| 分子式 | C19H23N9O | 分子量 | 393.45 |
| 溶解度 | DMF: 50 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 25 mg/ml,Ethanol: 10 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 | 2.5416 mL | 12.7081 mL | 25.4162 mL |
| 5 mM | 0.5083 mL | 2.5416 mL | 5.0832 mL |
| 10 mM | 0.2542 mL | 1.2708 mL | 2.5416 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet