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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.

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Lenalidomide Chemical Structure
Lenalidomide, CAS 191732-72-6
Pack Size Availability Price/USD Quantity
50 mg In stock $ 36.00
100 mg In stock $ 48.00
200 mg In stock $ 58.00
500 mg In stock $ 72.00
1 g In stock $ 98.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 99.52%
Purity: 99.5%
Purity: 98%
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Biological Description
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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

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

Solubility Information

DMSO: 25.9 mg/mL(100 mM)

TargetMolReferences 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.

TargetMolCitations

1. Durbin A D, Wang T, Wimalasena V K, et al. EP300 Selectively Controls the Enhancer Landscape of MYCN-Amplified NeuroblastomaEP300 Controls Enhancers and MYCN in Neuroblastoma. Cancer Discovery. 2022-12 (3) P730

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Hematonosis Compound Library Autophagy Compound Library Orally Active Compound Library FDA-Approved & Pharmacopeia Drug Library Approved Drug Library Pediatric Drug Library

Related Products

Related compounds with same targets
Naphthyridine carbamate dimer Lenalidomide hemihydrate dCeMM1 Mezigdomide Pomalidomide HQ461 FPFT-2216 Thalidomide

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Keywords

Lenalidomide 191732-72-6 Apoptosis PROTAC TNF Ligand for E3 Ligase Molecular Glues myeloma Inhibitor CRL4 ligase IKZF1 Ligands for E3 Ligase E3 ligase-recruiting Moiety immunomodulatory cereblon analog multiple CC5013 inhibit ligand CC 5013 IKZF3 degradation CC-5013 inhibitor

 

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