Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lenalidomide [191732-72-6]
Cat# T1642-1mL
Size : 1mL
Brand : TargetMol
Contact local distributor :
Phone : +1 850 650 7790
Lenalidomide
Catalog No. T1642 CAS 191732-72-6
Synonyms: CC-5013
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 products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Lenalidomide, CAS 191732-72-6
| 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. |
| Targets&IC50 | TNF-α:13 nM |
| 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]. |
| Synonyms | CC-5013 |
| Molecular Weight | 259.26 |
| Formula | C13H13N3O3 |
| CAS No. | 191732-72-6 |
Storage
Solubility Information
DMSO: 50 mg/mL (192.86 mM)
References and Literature
1. Kim K, et al. Lenalidomide induces apoptosis and alters gene expression in non-small cell lung cancer cells. Oncol Lett. 2013 Feb;5(2):588-592. 2. Lopez-Girona A, et al. Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide. Leukemia. 2012 Nov;26(11):2326-35. 3. Rozewski DM, et al. Pharmacokinetics and tissue disposition of lenalidomide in mice. AAPS J. 2012 Dec;14(4):872-82. 4. Dredge K, et al. Orally administered lenalidomide (CC-5013) is anti-angiogenic in vivo and inhibits endothelial cell migration and Akt phosphorylation in vitro. Microvasc Res. 2005 Jan;69(1-2):56-63. 6. Nagashima, Takeyuki, et al. PHARMACEUTICAL COMPOSITION COMPRISING BICYCLIC NITROGEN-CONTAINING AROMATIC HETEROCYCLIC AMIDE COMPOUND AS ACTIVE INGREDIENT. Patent. 20170360780A1.