Lenalidomide hydrochloride
Catalog No.
A3547
TNF-α分泌抑制剂
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IC50 Value: 13 nM [1]
Lenalidomideis a derivative of thalidomide introduced in 2004. Lenalidomide (Revlimid, CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM.
in vitro: Lenalidomide strongly induces IL-2 and sIL-2R production. Lenalidomide-induced tyrosine phosphorylation of CD28 on T cells is followed by a down-stream activation of NF-κB [2]. Lenalidomide and pomalidomide inhibits autoubiquitination of CRBN in HEK293 T cells expressing thalidomide-binding competent wild-type CRBN, but not thalidomide-binding defective CRBN (YW/AA). Overexpression of CRBN wild-type protein, but not CRBN (YW/AA) mutant protein, in KMS12 myeloma cells, amplifies pomalidomide-mediated reductions in c-myc and IRF4 expression and increases in p21(WAF-1) expression. Long-term selection for Lenalidomide resistance in H929 myeloma cell lines is accompanied by a reduction in CRBN, while in DF15R myeloma cells resistant to both pomalidomide and Lenalidomide, CRBN protein is undetectable [3].
in vivo: Pharmacokinetic studies evaluated doses of 0.5, 1.5, 5, and 10 mg/kg IV and 0.5 and 10 mg/kg doses for IP and oral routes. Liquid chromatography-tandem mass spectrometry was used to quantify lenalidomide in plasma, brain, lung, liver, heart, kidney, spleen, and muscle [4]. Treatment with either thalidomide or lenalidomide attenuated weight loss, enhanced motor performance, decreased motor neuron cell death, and significantly increased the life span in G93A transgenic mice [5].
Toxicity: International Staging System III received a combination therapy of lenalidomide (15 mg, Day 1 - 21) with dexamethasone (40 mg, Day 1, 8, 15, 22). After 4 days on chemotherapy, he experienced worsened dyspnea and was urgently hospitalized because of acute respiratory failure [6].
Clinical trial: Lenalidomide As Immune Adjuvant In Patient's With Chronic Lymphocytic Leukemia (CLL). Phase 2
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 295.72 |
Cas No. | 1243329-97-6 |
Formula | C13H14ClN3O3 |
Synonyms | Revlimid hydrochloride;CC-5013 hydrochloride;CC5013 hydrochloride;CC 5013 hydrochloride |
Solubility | insoluble in H2O; ≥1.83 mg/mL in EtOH; ≥72.2 mg/mL in DMSO |
Chemical Name | 3-(4-amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione hydrochloride |
SDF | Download SDF |
Canonical SMILES | O=C1N(C2C(NC(CC2)=O)=O)CC3=C(N)C=CC=C31.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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