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Lenalidomide

Cat. No. M1962

Lenalidomide Structure

Synonym: Revlimid, CC-5013

Size Price Availability Quantity
50mg USD 100 In stock
100mg USD 140 In stock
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Quality Control
Biological Activity

Lenalidomide (Revlimid) is a derivative of thalidomide. Lenalidomide has tumoricidal and immunomodulatory activity against multiple myeloma. Lenalidomide has also shown efficacy in the class of hematological disorders known as myelodysplastic syndromes (MDS). Lenalidomide maintenance therapy, initiated at day 100 after hematopoietic stem-cell transplantation, was associated with more toxicity and second cancers. Lenalidomide has significantly improved overall survival in myeloma (which generally carries a poor prognosis), although toxicity remains an issue for users.

Protocol
Cell Experiment
Cell lines HL60, MOLM13 and NB4 cells
Preparation method Spectrophotometric quantification of cell proliferation was assayed by the water soluble tetrazolium salt-1 (WST-1) (Roche Ltd, Basel, Switzerland) based colorimetric assay. This tetrazolium salt is reduced extracellularly to formazan dye by enzymes of the plasma membrane oxidoreductase. (122) The primary reductant is NADH derived from the TCA of the mitochondria. Hence, WST-1 is converted by metabolically active cells and was employed to measure cell proliferation. The cell lines HL60, MOLM13 and NB4 were plated in triplicate (20×103 cells/well) in a 96-well microplate and treated with either LND (1, 5, 20, 50, 100, 200, and 500 µM) .
Concentrations 1, 5, 20, 50, 100, 200, and 500 µM
Incubation time 48 h
Animal Experiment
Animal models NOD/scid/gamma (NSG) mice
Formulation 10% DMSO, 70% PEG300
Dosages 50 mg/kg daily
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 259.26
Formula C13H13N3O3
CAS Number 191732-72-6
Purity >99%
Solubility DMSO 52 mg/mL
Storage at -20°C
Customer Product Validation
Source Int Immunopharmacol (2015). Lenalidomide, Figure 9. (AbMole BioScience, Houston, TX, USA)
Method MTT assay
Cell Lines BV-2 cells
Concentrations 10 μM
Incubation Time 30 min
Results Lenalidomide significantly decreased hypoxia-induced mRNA levels of TNF-alpha (Fig. 9A). Next to determine whether the inhibition of TNF-alpha contributes to microglial-CM induced neuron death, BV-2 cells were pretreated with lenalidomide (10 μM) for 30 min, and then exposed hypoxia for 24 h; neuronal cells were treated with different CM from BV-2 cells for 24 h. MTT assay showed that the viability of neurons in the hypoxia-CM condition was significantly decreased, while this effect was reversed by the CM treated with hypoxia and lenalidomide (Fig. 9B).
Rating
Source Graduation Thesis (2015) . Figure 14.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2)
Method hochest staining and Annexin-V/PI flow cytometry
Cell Lines HL60, MOLM13 and NB4 cells
Concentrations 1, 5, 20, 50, 100 µM
Incubation Time 48 h
Results An overall higher degree of reduced metabolic activity was observed from three independent studies with MOLM13 (Figure 14A) and NB4 (Figure 14B) cells thus were suggested being more responsive to co-treatment.
Rating
Source Graduation Thesis (2015) . Figure 13.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2)
Method hochest staining and Annexin-V/PI flow cytometry
Cell Lines HL60, MOLM13 and NB4 cells
Concentrations 1, 5, 20, 50, 100 µM
Incubation Time 48 h
Results These data indicated a comparable trend of viability in all three cell lines following combinatorial treatment of VPA and LND (Figure 13B, C). HL60 cells are only presented for Hoechst viability scoring in figure 13A since the cells do not expose phosphatidylserine upon apoptosis induction.
Rating
Source Graduation Thesis (2015) . Figure 12.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2)
Method WST-1 proliferation based assay
Cell Lines HL60 cells
Concentrations 50, 100 µM
Incubation Time 48 h
Results Maximal potentiation of LND was obtained by 100 µM LND in the sequence VPA→LND+VPA, but no significant increased anti-proliferative effect was obtained from three independent and replicable studies.
Rating
Source Graduation Thesis (2015) . Figure 11.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2)
Method Hochest staining
Cell Lines HL60, MOLM13 and NB4 cells
Concentrations 1 µM ~ 500 µM
Incubation Time 24 h and 48 h
Results The frequencies of abnormal nucleic morphology were minor at concentrations lower than 50 µM in all three cell lines.
Rating
Source Graduation Thesis (2015) . Figure 10.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2)
Method WST-1 proliferation based assay
Cell Lines HL60, MOLM13 and NB4 cells
Concentrations 20 µM ~ 500 µM
Incubation Time 48 h
Results The IC50 of LND in NB4 (201 µM), HL60 (248 µM) and MOLM13 (124 µM) are presented in Figure 10 B, C and D indicating LND to be more effective after 48 hour treatment in MOLM13 and NB4 cells at lower concentrations than when treated for 24 hours.
Rating
Source Graduation Thesis (2015) . Figure 9.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2)
Method WST-1 proliferation based assay
Cell Lines HL60, MOLM13 and NB4 cells
Concentrations HL60 (149 µM, CI: 110-200 µM), MOLM13 (218 µM, CI: 153 – 311 µM), and NB4 (203µM, CI: 106 – 387 µM)
Incubation Time 24 h
Results IC50s of LND was obtained from WST-1 proliferation assay, and are presented in Figure 9B, C and D for HL60 (149 µM), MOLM13 (218 µM) and NB4 (203 µM), respectively.
Rating
Source Graduation Thesis (2015) . Figure 7.Lonidamine (AbMole BioScience, CAS No.: 50264-69-2)
Method WST-1 proliferation based assay
Cell Lines NB4 cells
Concentrations 12.5, 25, 50, 75, 100 µ M
Incubation Time 48 h
Results the combination of LND and MMF neither showed significant enhanced potentiation of MMF nor LND.
Rating
Product Citations
References

Lenalidomide after stem-cell transplantation for multiple myeloma.
McCarthy PL, et al. N Engl J Med. 2012 May 10;366(19):1770-81. PMID: 22571201.

Continuous lenalidomide treatment for newly diagnosed multiple myeloma.
Palumbo A, et al. N Engl J Med. 2012 May 10;366(19):1759-69. PMID: 22571200.

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Keywords: Lenalidomide, Revlimid, CC-5013 supplier, TNF-alpha, inhibitors

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