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别名 | K17 | 储存条件 (自收到货起) |
3年 / -20°C / 粉状 1年 / -80°C / 溶于溶剂 |
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化学式 | C13H10N2O4 |
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分子量 | 258.23 | CAS号 | 50-35-1 | |
Solubility (25°C)* | 体外 | DMSO | 52 mg/mL (201.37 mM) | |
Ethanol | 2 mg/mL (7.74 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
产品描述 | Thalidomide作为一种镇静药,免疫调节剂,也用于研究治疗许多癌症的症状。沙利度胺能够抑制cereblon (CRBN),它是cullin-4 E3 泛素连接酶复合物CUL4-RBX1-DDB1的一部分。 | ||
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体外研究 | Thalidomide必须通过肝脏代谢以形成环氧化物,可能是活性致畸代谢物。[1] Thalidomide选择性地抑制脂多糖和其他激动剂刺激人体单核细胞生产肿瘤坏死因子α(TNF-α)。[2] Thalidomide通过增强mRNA降解发挥其对肿瘤坏死因子α的抑制作用。[3] Thalidomide通过诱导细胞凋亡和G1期生长停滞直接作用在MM细胞系以及抗melphalan, doxorubicin和dexamethasone 的病人的MM细胞。Thalidomide增强塞米松的抗MM活性,而白介素6会抑制其活性。[4] Thalidomide是原代人T细胞在体外的有力协同刺激分子,通过T细胞受体复合物以协同增加白细胞介素-2介导的T细胞增殖和干扰素γ生成。Thalidomide也增加在不存在的CD4 + T细胞的同种异体树突状细胞诱导初级CD8 +细胞毒性T细胞应答。[5] |
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体内研究 | Thalidomide(200 毫克/千克)导致在兔子体内血管化角膜区的抑制,抑制率在三个实验中从30%到51%,抑制率中位数为36%。[1] |
数据来源于[Data independently produced by , , Blood, 2017, 129(10):1308-1319]
数据来源于[Data independently produced by , , FASEB Journal, 2015, fj.15-274050]
数据来源于[Data independently produced by , , Oncotarget, 2016, 7(25):38539-38550]
数据来源于[Data independently produced by , , J Immunol Res, 2018, 2018:5070573]
A small-molecule degrader selectively inhibits the growth of ALK-rearranged lung cancer with ceritinib resistance [ iScience, 2024, 27(2):109015.] | PubMed: 38327793 |
Lenalidomide bypasses CD28 co-stimulation to reinstate PD-1 immunotherapy by activating Notch signaling [ Cell Chem Biol, 2022, S2451-9456(22)00204-5] | PubMed: 35732177 |
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] | PubMed: 35207746 |
Establishment and characterization of NCC-UPS4-C1: a novel cell line of undifferentiated pleomorphic sarcoma from a patient with Li-Fraumeni syndrome [ Hum Cell, 2022, 10.1007/s13577-022-00671-y] | PubMed: 35118583 |
Establishment and characterization of the NCC-GCTB4-C1 cell line: a novel patient-derived cell line from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00639-4] | PubMed: 34731453 |
Establishment and characterization of NCC-MFS4-C1: a novel patient-derived cell line of myxofibrosarcoma [ Hum Cell, 2021, 34(6):1911-1918] | PubMed: 34383271 |
Establishment and characterization of novel patient-derived cell lines from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00579-z] | PubMed: 34304386 |
Protein Ligand Interactions Using Surface Plasmon Resonance [ Methods Mol Biol, 2021, 2365:3-20] | PubMed: 34432236 |
Evaluation of the binding affinity of E3 ubiquitin ligase ligands by cellular target engagement and in-cell ELISA assay [ STAR Protoc, 2021, 2(1):100288] | PubMed: 33532735 |
Evaluation of the binding affinity of E3 ubiquitin ligase ligands by cellular target engagement and in-cell ELISA assay [ STAR Protoc, 2021, 2(1):100288] | PubMed: 33532735 |
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如果需要长期保存,请于零下二十度低温保存。禁止用于人体及治疗!
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