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Pomalidomide-d5
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pomalidomide-d5图片
规格:98%
分子量:278.3
包装与价格:
包装价格(元)
500ug电议
1mg电议

产品介绍
Pomalidomide-d5 是氘标记的 Pomalidomide。第三代免疫调节剂泊马度胺起到分子胶的作用。 Pomalidomide 与 E3 连接酶 cereblon 相互作用并诱导基本 Ikaros 转录因子的降解。
货号:ajcx23286
CAS:1377838-49-7
分子式:C13H6D5N3O4
分子量:278.3
溶解度:DMF: 10 mg/ml,DMSO: 15 mg/ml
纯度:98%
存储:Store at -20°C
库存:现货

Background:

Pomalidomide-d5is 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 IC50value of approximately 3 µM for the human recombinant CRBN-DNA damage binding protein-1 (CRBN-DDB1) complex.1It 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-8.2,3Pomalidomide (3 mg/kg per day), in combination with dexamethasone, reduces tumor growth in a H929 R10-1 lenalidomide-resistant mouse xenograft model.4Formulations 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)