This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
Lenalidomide hydrochloride
Catalog No. T21763 CAS
1243329-97-6
Lenalidomide hydrochloride (CC-5013 hydrochloride), a Thalidomide derivative, functions as molecular glue and serves as an orally active immunomodulator. As a ligand for the ubiquitin E3 ligase cereblon (CRBN), it facilitates the selective ubiquitination and degradation of the lymphoid transcription factors IKZF1 and IKZF3 through the CRBN-CRL4 ubiquitin ligase. Specifically, Lenalidomide hydrochloride inhibits the growth of mature B-cell lymphomas, including multiple myeloma, and promotes IL-2 release from T cells [1] [2].
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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Biological Description
Chemical Properties
Storage
& Solubility Information
Description
Lenalidomide hydrochloride (CC-5013 hydrochloride), a Thalidomide derivative, functions as molecular glue and serves as an orally active immunomodulator. As a ligand for the ubiquitin E3 ligase cereblon (CRBN), it facilitates the selective ubiquitination and degradation of the lymphoid transcription factors IKZF1 and IKZF3 through the CRBN-CRL4 ubiquitin ligase. Specifically, Lenalidomide hydrochloride inhibits the growth of mature B-cell lymphomas, including multiple myeloma, and promotes IL-2 release from T cells [1] [2].
In vitro
Lenalidomide, a thalidomide analog, is effective in enhancing T cell proliferation and the production of IFN-γ and IL-2, while simultaneously inhibiting the generation of pro-inflammatory cytokines (TNF-α, IL-1, IL-6, IL-12) and increasing anti-inflammatory IL-10 levels in human PBMCs. It directly reduces IL-6 production and disrupts the interaction between multiple myeloma (MM) cells and bone marrow stromal cells (BMSC), leading to increased apoptosis of myeloma cells. Furthermore, lenalidomide, along with Thalidomide and Pomalidomide, demonstrates a dose-dependent interaction with the CRBN-DDB1 complex, showing specificity in inhibiting cell proliferation, particularly in cells expressing reduced levels of CRBN. Notably, lenalidomide acts as a molecular bridge promoting the ubiquitination and degradation of CKIα by facilitating its connection with the cereblon E3 ubiquitin ligase, potentially activating p53 to target leukemic cells for destruction.
In vivo
Lenalidomide, administered through intravenous (IV), intraperitoneal (IP), and oral (PO) routes at doses up to 15 mg/kg, 22.5 mg/kg, and 45 mg/kg, demonstrates acceptable toxicity profiles. The compound's solubility in a Phosphate Buffered Saline (PBS) dosing vehicle constrains the maximum doses. Despite this limitation, the doses are generally well tolerated, except for a single mortality observed in one mouse (of four total dosed) at the 15 mg/kg IV dosage. No additional toxicities were noted at IV doses of 15 mg/kg (n=3) or 10 mg/kg (n=45), nor at any levels across the studied administration routes [4].
Molecular Weight
295.72
Formula
C13H14ClN3O3
CAS No.
1243329-97-6
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dose Conversion
You can also refer to dose conversion for different animals.
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Method for preparing DMSO master liquid: mg
drug pre-dissolved in μL DMSO (Master liquid concentration
mg/mL),
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL PEG300, mix and clarify, next add μL
Tween 80,mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL Corn oil,mix and clarify.
Note:
Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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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.