来那度胺半水合物
中文名称 | 来那度胺半水合物 |
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中文同义词 | 来那度胺半水合物;TNF-Α分泌抑制剂 |
英文名称 | LenalidoMide (heMihydrate) |
英文同义词 | LenalidoMide (heMihydrate);Lenalidomide hemihydrate (Revlimid, CC 5013);CC-5013 hemihydrate;Lenalidonmide;IKZF3,inhibit,IKZF1,ligand,Inhibitor,CC-5013 hemihydrate,degradation,myeloma,Ligands for E3 Ligase,analog,multiple,Lenalidomide hemihydrate,immunomodulatory,E3 ligase-recruiting Moiety,CRL4,ligase,Molecular Glues,cereblon,Apoptosis;3-(4-Amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione hemihydrate |
CAS号 | 847871-99-2 |
分子式 | C26H28N6O7 |
分子量 | 536.53652 |
EINECS号 | |
相关类别 | 细胞生物学试剂;原料药;原料药-API;原料药 |
Mol文件 | 847871-99-2.mol |
结构式 |
来那度胺半水合物 性质
储存条件 | Store at -20°C |
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溶解度 | DMSO : 50 mg/mL (186.38 mM; 需要超声波)H2O : < 0.1 mg/mL (不溶) |
形态 | 粉末 |
颜色 | 米白色至粉红色 |
InChI | InChI=1S/2C13H13N3O3.H2O/c2*14-9-3-1-2-7-8(9)6-16(13(7)19)10-4-5-11(17)15-12(10)18;/h2*1-3,10H,4-6,14H2,(H,15,17,18);1H2 |
InChIKey | OTJHSDXKMBRCMM-UHFFFAOYSA-N |
Cereblon
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Lenalidomide is potent in stimulating T cell proliferation and IFN-γ and IL-2 production. Lenalidomide has been shown to inhibit production of pro inflammatory cytokines TNF-α, IL-1, IL-6, IL-12 and elevate the production of anti-inflammatory cytokine IL-10 from human PBMCs. Lenalidomide downregulates the production of IL-6 directly and also by inhibiting multiple myeloma (MM) cells and bone marrow stromal cells (BMSC) interaction, which augments the apoptosis of myeloma cells. Dose-dependent interaction with the CRBN-DDB1 complex is observed with Thalidomide, Lenalidomide and Pomalidomide, with IC 50 values of ~30 μM, ~3 μM and ~3 μM, respectively, These reduced CRBN expression cells (U266-CRBN 60 and U266-CRBN 75 ) are less responsive than the parental cells to antiproliferative effects Lenalidomide across a dose-response range of 0.01 to 10 μM. Lenalidomide, a thalidomide analog, functions as a molecular glue between the human E3 ubiquitin ligase cereblon and CKIα is shown to induce the ubiquitination and degradation of this kinase, thus presumably killing leukemic cells by p53 activation.
The toxicity of Lenalidomide doses up to 15, 22.5, and 45 mg/kg via IV, IP, and PO routes of administration. Limited by solubility in our PBS dosing vehicle, these maximum achievable Lenalidomide doses are well tolerated with the exception of one mouse death (of four total dosed) at the 15 mg/kg IV dose. Notably, no other toxicities are observed in the study at IV doses of 15 mg/kg (n=3) or 10 mg/kg (n=45) or at any other dose level through IV, IP, and PO routes.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/04/30 | HY-A0003B | 来那度胺半水合物 Lenalidomide hemihydrate | 847871-99-2 | 100 mg | 1350元 |
2024/04/30 | HY-A0003B | 来那度胺半水合物 Lenalidomide hemihydrate | 847871-99-2 | 10mM * 1mLin DMSO | 1485元 |