来那度胺 T1642

Product Introduction
Bioactivity


英文名: Lenalidomide

描述: Lenalidomide (CC-5013) 是 Thalidomide 的衍生物，也是具有口服活性免疫调节剂，以分子胶的方式作用。它是泛素 E3 连接酶 cereblon (CRBN) 的配体，可通过 CRBN-CRL4 泛素连接酶对两种淋巴转录因子 IKZF1 和 IKZF3 进行选择性泛素化和降解。

细胞实验: The human NSCLC cell lines Lu-99, H1299, A549, EBC1, and H460 were cultured in RPMI-1640 medium containing 10% fetal bovine serum and antibiotics at 37°C in a humidified chamber containing 5% CO2. Cells were seeded into 60-mm culture dishes (2x10^5 cells per dish) with various concentrations of lenalidomide and incubated for various times [1].

动物实验: Mice were administered sterile preparations of lenalidomide normalized to body weight. Intravenously (IV) dosed animals received drug by bolus tail vein injections, and extravascularly dosed mice received drug by bolus intraperitoneal injections (IP) or oral gavage (PO). Dosing solution, concentrations were adjusted so dose volumes ranged between approximately 100 and 150 μL for IV injections and between approximately 150 and 250 μL for IP and PO dosing in the pharmacokinetic study. However, for the range-finding study, increased dose volumes were used (up to 200 μL IV, 300 μL IP, and 600 μL PO, per approved animal use protocol) to explore elevated lenalidomide doses. The bolus injection rates for all IV, IP, or PO injections were less than 5 s. Concentrations of dosing solutions were verified by liquid chromatography-mass spectrometry [4].

体外活性: Lenalidomide significantly inhibited the proliferation of NSCLC cells (Lu-99, H1299, H460 and A549) in a concentration-dependent manner. In particular, H460 cells had the highest sensitivity for lenalidomide. 3-fold more mRNAs were downregulated (474 mRNAs) than upregulated (158 mRNAs) by lenalidomide (10 μM) treatment in H460 cells [1]. The ubiquitously expressed E3 ligase protein cereblon (CRBN) mediated antiproliferative activities of lenalidomide in myeloma cells, as well as lenalidomide-induced cytokine production in T cells. Lenalidomide inhibited autoubiquitination of CRBN in HEK293T cells expressing thalidomide-binding competent wild-type CRBN, but not thalidomide-binding defective CRBN(YW/AA) [2].

体内活性: Doses of 15 mg/kg IV, 22.5 mg/kg IP, and 45 mg/kg PO lenalidomide caused no observable toxicity up to 24 h postdose. Administration of 0.5 and 10 mg/kg resulted in systemic bioavailability ranges of 90-105% and 60-75% via IP and oral routes, respectively. Lenalidomide was detectable in the brain only after IV dosing of 5 and 10 mg/kg [3]. Oral administration of lenalidomide attenuates growth factor-induced angiogenesis in vivo; the rat mesenteric window assay was utilized to show that lenalidomide significantly inhibits vascularization in a dose-dependent manner [4].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (192.86 mM)
5% DMSO+95% Saline : 1.3 mg/mL (4.99 mM, suspension)


关键字: myeloma | Inhibitor | CRL4 | ligase | IKZF1 | Ligands for E3 Ligase | E3 ligase-recruiting Moiety | Apoptosis | immunomodulatory | cereblon | analog | multiple | CC5013 | inhibit | ligand | Lenalidomide | CC 5013 | IKZF3 | Molecular Glues | degradation

相关产品: (S,R,S)-AHPC TFA | HaloPROTAC3 | Thalidomide-O-amido-C6-NH2 TFA | BSJ-4-116 | Lenalidomide hemihydrate | CFT7455 | (S,R,S)-AHPC-PEG2-NH2 dihydrochloride | Thalidomide-NH-CH2-COOH | Pomalidomide-C2-NH2 hydrochloride | Pomalidomide

相关库: Drug Repurposing Compound Library | Angiogenesis related Compound Library | Anti-Cancer Drug Library | Bioactive Compounds Library Max | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Preclinical Compound Library | Anti-Cardiovascular Disease Compound Library

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