Pomalidomide-d5
(Synonyms: 泊马度胺杂质,CC-4047-d5) 目录号 : GC47965An internal standard for the quantification of pomalidomide
Cas No.:1377838-49-7
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Pomalidomide-d5 is intended for use as an internal standard for the quantification of pomalidomide by GC- or LC-MS. Pomalidomide is an analog of thalidomide that inhibits the E3 ligase protein cereblon (CRBN) with an IC50 value of approximately 3 µM for the human recombinant CRBN-DNA damage binding protein-1 (CRBN-DDB1) complex.1 It inhibits autoubiquitination of CRBN in HEK293T cells expressing CRBN but not those expressing a thalidomide-binding defective CRBN mutation. It inhibits proliferation of U266 myeloma cells when used at concentrations ranging from 0.1 to 10 µM. Pomalidomide also has antiangiogenic and immunomodulatory effects against myeloma cells, modulating cell adhesion, decreasing production of key pro-survival cytokines, including TNF-α, and triggering the activation of caspase-8.2,3 Pomalidomide (3 mg/kg per day), in combination with dexamethasone, reduces tumor growth in a H929 R10-1 lenalidomide-resistant mouse xenograft model.4 Formulations containing pomalidomide have been used in the treatment of multiple myeloma.
1.Lopez-Girona, A., Mendy, D., Miller, K., et al.Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomideLeukemia26(11)2326-2335(2012) 2.Zhu, Y.X., Kortuem, K.M., and Stewart, A.K.Molecular mechanism of action of immune-modulatory drugs thalidomide, lenalidomide and pomalidomide in multiple myelomaLeukemia and Lymphoma54(4)683-687(2013) 3.Latif, T., Chauhan, N., Khan, R., et al.Thalidomide and its analogues in the treatment of multiple myelomaExp.Hermatol.Oncol.1(1)27(2012) 4.Rychak, E., Mendy, D., Shi, T., et al.Pomalidomide in combination with dexamethasone results in synergistic anti-tumour responses in pre-clinical models of lenalidomide-resistant multiple myelomaBr. J. Haematol.172(6)889-901(2016)
Cas No. | 1377838-49-7 | SDF | |
别名 | 泊马度胺杂质,CC-4047-d5 | ||
Canonical SMILES | NC1=C2C(C(N(C3([2H])C(NC(C([2H])([2H])C3([2H])[2H])=O)=O)C2=O)=O)=CC=C1 | ||
分子式 | C13H6D5N3O4 | 分子量 | 278.3 |
溶解度 | DMF: 10 mg/ml,DMSO: 15 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.5932 mL | 17.9662 mL | 35.9324 mL |
5 mM | 0.7186 mL | 3.5932 mL | 7.1865 mL |
10 mM | 0.3593 mL | 1.7966 mL | 3.5932 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。