Lenalidomide

SKU: orb1307920

Description

Lenalidomide

Research Area

Cell Biology, Immunology & Inflammation, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 191732-72-6
• MW: 259.26
• Purity: 99.50%
• Formula: C₁₃H₁₃N₃O₃
• SMILES: NC1=C2CN(C3CCC(=O)NC3=O)C(=O)C2=CC=C1
• Target: Apoptosis,IKZF,TNF,Ligand for E3 Ligase,Molecular Glues
• Solubility: DMSO:125 mg/mL (482.14 mM);10% DMSO+90% Saline:2.6 mg/mL (10.03 mM)

Bioactivity

• Target IC50:
  TNF-α:13 nM|HMCL ALMC-1 cells viability:2.6 μM|MM.1S cells proliferation:81 nM
• In Vivo:
  METHODS: To tes the antitumor activity in vivo Lenalidomide (25 mg/kg) was injected intraperitoneally into C57BL/KaLwRij or B6-SCID mice bearing 5TGM1 tumors once daily for 21 days. RESULTS: Lenalidomide inhibited tumor growth and prolonged survival of C57BL/KaLwRij mice bearing 5TGM1 tumors.Lenalidomide significantly increase the number of IFN-γ-secreting CD4+ and CD8+ T cells but had no effect on NK cells and B cells in the B6-SCID mouse model. Lenalidomide slightly decrease the number of CD25+Foxp3+ T cells in vivo but increased perforin expression in CD8+ T cells.Lenalidomide promoted type 1 antitumor immune responses in vivo
• In Vitro:
  METHODS: Six malignant glioma cell lines, A-172, AM-38, T98G, U-138MG, U-25 mg, and YH-13, were treated with Lenalidomide (0.01-100 µM) for 72 h, and cell counts were detected by Coulter counter assay. Results: Lenalidomide inhibited cell counts of All malignant glioma cells in a concentration dependent manner. METHODS: DCs were differentiated from BM CD14+ cells from mM patients, treated with Lenalidomide (0.1-1 µM) for 8 days and analyzed for DC maturation markers by flow-cytometry. Results: Despite a reduction in the number and percentage of mature DCs, Lenalidomide significantly increase the expression of HLA-DR, CD86, and CD209 in DCs derived from BM ove the range of concentration achieved in mM patients.
• 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℃n a humidified chamber containing 5% CO2. Cells were seeded into 60 mM culture dishes (2x10^5 cells per dish) with various concentration of lenalidomide and incubated for various times.
• 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, concentration 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, fo 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. concentration of dosing solutions were verified by liquid chromatography-mass spectrometry .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

analog, Apoptosis, cereblon, CC5013, CC-5013, CC 5013, degradation, CRL4, E3 ligase-recruiting Moiety, MolecularGlues, Molecular Glues, inhibit, immunomodulatory, multiple, myeloma, Ligand for E3 Ligase, LigandforE3Ligase, Ligands for E3 Ligase, ligase, ligand, Inhibitor, IKZF3, IKZF1, Lenalidomide, TNF-α

Compound Identifiers

PubChem CID

216326