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Lenalidomide

Lenalidomide
Lenalidomide (CC-5013) is an immunomodulator with oral activity. Lenalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN), which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase, and is commonly used in the synthesis of PROTAC products.
Catalog No. T1642Cas No. 191732-72-6
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Purity:99.97%
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Lenalidomide

Catalog No. T1642Cas No. 191732-72-6

Lenalidomide (CC-5013) is an immunomodulator with oral activity. Lenalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN), which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase, and is commonly used in the synthesis of PROTAC products.
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 SizePriceAvailabilityQuantity
50 mg$36In Stock
100 mg$48In Stock
200 mg$58In Stock
500 mg$72In Stock
1 g$98In Stock
1 mL x 10 mM (in DMSO)$50In Stock
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Product Introduction

Bioactivity
Description
Lenalidomide (CC-5013) is an immunomodulator with oral activity. Lenalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN), which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase, and is commonly used in the synthesis of PROTAC products.
Targets&IC50
TNF-α:13 nM
In vitro
METHODS: Six malignant glioma cell lines, A-172, AM-38, T98G, U-138MG, U-251MG, 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. [1]
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 increased the expression of HLA-DR, CD86, and CD209 in DCs derived from BM over the range of concentrations achieved in MM patients. [2]
In vivo
METHODS: To test 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 increased 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 decreased 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. [3]
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].
AliasCC-5013
Chemical Properties
Molecular Weight259.26
FormulaC13H13N3O3
Cas No.191732-72-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (192.86 mM)
10% DMSO+90% Saline: 2.59 mg/mL (9.99 mM), Working solution is recommended to be prepared and used immediately.
Solution Preparation Table
10% DMSO+90% Saline/DMSO
1mg5mg10mg50mg
1 mM3.8571 mL19.2857 mL38.5713 mL192.8566 mL
5 mM0.7714 mL3.8571 mL7.7143 mL38.5713 mL
DMSO
1mg5mg10mg50mg
10 mM0.3857 mL1.9286 mL3.8571 mL19.2857 mL
20 mM0.1929 mL0.9643 mL1.9286 mL9.6428 mL
50 mM0.0771 mL0.3857 mL0.7714 mL3.8571 mL
100 mM0.0386 mL0.1929 mL0.3857 mL1.9286 mL

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