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.
Blood. 2021 Dec 23;138(25):2655-2669.
Targeting intracellular WT1 in AML with a novel RMF-peptide-MHC specific T-cell bispecific antibody
Lenalidomide purchased from AbMole
BMC Biol. 2021 May 20;19(1):108.
Very long intergenic non-coding (vlinc) RNAs directly regulate multiple genes in cis and trans
Lenalidomide purchased from AbMole
Int Immunopharmacol. 2015 Sep;578-87.
Resveratrol attenuates hypoxia-induced neurotoxicity through inhibiting microglial activation.
Lenalidomide purchased from AbMole
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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). |
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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. |
 |
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. |
 |
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. |
 |
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. |
 |
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. |
 |
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. |
 |
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. |
| 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. |
| Molecular Weight | 259.26 |
| Formula | C13H13N3O3 |
| CAS Number | 191732-72-6 |
| Solubility (25°C) | DMSO 34 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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