Lenalidomide [191732-72-6]
Cat# T1642-1mL
Size : 1mL
Brand : TargetMol
Lenalidomide
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Purity:99.52%
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COA HNMR HPLC
Lenalidomide
Catalog No. T1642Cas No. 191732-72-6
Lenalidomide (CC-5013) is a potent inhibitor of TNF-α that, at 10 μM, alters gene expression and cell viability in a range of cancer cell lines.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. Pack Size | |
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50 mg | |
100 mg | |
200 mg | |
500 mg | |
1 g | |
1 mL x 10 mM (in DMSO) |
Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
Description | Lenalidomide (CC-5013) is a potent inhibitor of TNF-α that, at 10 μM, alters gene expression and cell viability in a range of cancer cell lines. |
In vitro | 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]. |
In vivo | 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]. |
Cell Research | 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]. |
Animal Research | 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]. |
Alias | CC-5013 |
Molecular Weight | 259.26 |
Formula | C13H13N3O3 |
Cas No. | 191732-72-6 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (192.86 mM) 5% DMSO+95% Saline: 1.3 mg/mL (4.99 mM, precipitation) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
DMSO/5% DMSO+95% Saline
DMSO
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg,each animal weighs 20 g, and the dosage volume is 100 μL. A total of 10 animals were administered, and the formula you used is 5% DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL.
Mother liquor preparation method: 2 mg of drug dissolved in 50 μLDMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μLDMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μLTween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify.
Dose Conversion
You can also refer to dose conversion for different animals. More
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Keywords
myelomaInhibitorCRL4ligaseIKZF1Ligands for E3 LigaseE3 ligase-recruiting MoietyApoptosisimmunomodulatorycereblonanalogmultipleCC5013inhibitligandLenalidomideCC 5013IKZF3Molecular Gluesdegradation