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CAS NO.191732-72-6
98%(500-1000)Kilogram98%(100-500)Metric Ton
| Molecular Formula | C13H13N3O3 |
| Molar Mass | 259.26 |
| Density | 1.460±0.06 g/cm3(Predicted) |
| Melting Point | 265-268 °C |
| Boling Point | 614.0±55.0 °C(Predicted) |
| Flash Point | 325.1°C |
| Solubility | Soluble in DMSO (≥52 mg/ml) at 25 °C, methanol and water (2: 1), buffered aqueous sol |
| Vapor Presure | 5.2E-15mmHg at 25°C |
| Appearance | Solid |
| Color | White |
| pKa | 10.75±0.40(Predicted) |
| Storage Condition | 2-8°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Refractive Index | 1.672 |
| Use | A Thalidomide analog known to have immunomodulatory properties |
| In vitro study | CC-5013 strong induction IL-2 and sIL-2R yield. CC-5013 acts on T cells to induce tyrosine phosphorylation of CD28 and subsequently down-regulate activation of NF-κB. Lenalidomide and Pomalidomide act on HEK293 T cells expressing wild-type CRBN bound to Thalidomide, but not Thalidomide bound to defective CRBN(YW/AA), to inhibit CRBN autoubiquitination. In KMS12 multiple myeloma cells, overexpression of the CRBN wild-type protein but not the CRBN(YW/AA) mutant protein amplifies Pomalidomide-regulated c-myc and decreases in IRF4 expression and increases in p21(WAF-1) expression. The selectivity of long-term resistance to Lenalidomide in H929 multiple myeloma cell lines was associated with decreased CRBN, whereas no CRBN protein was detected in DF15R multiple myeloma resistant to Pomalidomide and Lenalidomide. Lenalidomide inhibits the development of defects by down-regulating the expression of tumor cell inhibitory molecules. Lenalidomide prevents tumor-induced T-cell lytic dysfunction from occurring. Lenalidomide acts on T cells to inhibit chronic lymphocytic leukemia (CLL) cell-induced impairment of T cell actin synaptic function, and down-regulates CLL to inhibit the expression of ligands and other receptors. Lenalidomide acts on FL, DLBCL, HL, MM, SCC, and OC, inhibits tumor-induced immunosuppression, and down-regulates immunosuppressive ligand expression when it acts on all tumor cells tested. |
| In vivo study | Oral treatment of Lenalidomide significantly inhibited bFGF-induced angiogenesis in a dose-dependent manner. Lenalidomide significantly reduced percent vascular area from 5.16 percent in the control group to 2.58(50 mg/kg treatment) and 1.69(250 mg/kg treatment) in the experimental group. Lenalidomide significantly reduced overall MVL from 21.07 in the control group to 8.11(50 mg/kg dose treatment) and 1.90(250 mg/kg dose treatment) in the experimental group. |
| Introduction | In the past ten years, lenalidomide (also known as ralidomide) has been successfully used to treat inflammatory diseases and cancer. The indications approved by FDA are: combined dexamethasone for the treatment of multiple myeloma (MM); As a maintenance treatment after receiving autologous hematopoietic stem cell transplantation. However, what many patients and friends do not know is that it can also be used in hepatocellular carcinoma. |
| mechanism of action | lenalidomide is an immunomodulatory drug, which has a variety of mechanisms of action. in vitro studies, lenalidomide has three main effects: 1) direct anti-tumor effect 2) inhibition of angiogenesis 3) immune regulation. In vivo, lenalidomide directly or indirectly induces apoptosis of tumor cells by inhibiting the supportive, anti-angiogenic and anti-osteoclast effects of bone marrow stromal cells, as well as immunomodulatory activity. At the molecular level, lenalidomide has been shown to interact with the ubiquitin E3 ligase and target this enzyme to degrade the Ikaros transcription factors IKZF1 and IKZF3. |
| anti-tumor drug | lenalidomide is an anti-tumor drug developed by Celgene biopharmaceutical company in the United States. Its chemical structure is similar to thalidomide and has multiple effects such as anti-tumor, immune regulation and anti-angiogenesis. It can inhibit the secretion of proinflammatory cytokines and increase the secretion of anti-inflammatory cytokines from peripheral blood mononuclear cells. In vitro tests show that this product can inhibit the proliferation of some cell lines such as Namalwa cells. Lenalidomide can inhibit the growth of multiple myeloma cells and MM1S cells in patients. In addition, this product can also inhibit the expression of cyclooxygenase-2 (COX-2), but has no effect on COX-1. Two multi-center randomized blind placebo-controlled clinical studies evaluated the safety and efficacy of lenalidomide in multiple myeloma. The main efficacy endpoints of the study were time to disease progression (TTP). The interim analysis showed that TTP in the combination group was significantly better than that in the dexamethasone monotherapy group. Recent clinical research results show that lenalidomide can not only be used to treat MDS and MM, but also has certain curative effect on myeloma, leukemia, metastatic kidney cancer, solid tumor, primary systemic starch degeneration and systemic myelofibrosis with bone marrow metaplasia. lenalidomide is a new generation derivative of thalidomide, but it has not been found to have teratogenic toxicity, and its efficacy is 100 times stronger than thalidomide. According to the results of phase III clinical trials, lenalidomide is currently the most effective drug in the treatment of multiple myeloma. More than half of patients can prolong their survival time by more than 3 years after taking the drug. In addition, it is also the only drug that can effectively treat myelodysplastic syndrome (MDS). Clinical results show that 64% MDS patients do not need to use blood transfusion to treat MDS after nalidomide treatment. In December 2005, the U.S. Food and Drug Administration (FDA) approved lenalidomide for the treatment of myelodysplastic syndrome (MDS). in March 2006, FDA approved lenalidomide produced by Celgene biopharmaceutical company in the United States for the treatment of multiple myeloma (MM). On September 23, 2011, the European Medicines Agency (EMA) released information that it has confirmed that the benefits of lenalidomide (trade name: Revlimid) in its approved patient population outweigh the risks, but it also warned doctors about the risk of new cancers caused by the drug. Lenalidomide in combination with dexamethasone is used to treat adult patients with multiple myeloma who have received at least one treatment before. Three new studies have shown an increased incidence of new cancers in patients with newly diagnosed multiple myeloma who receive both lenalidomide and other combinations. |
| Biological activity | Lenalidomide (CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand ubiquitin E3 ligase cereblon (CRBN), which causes selective ubiquitination and degradation of two lymphoid transcription factors IKZF1 and IKZF3 by CRBN-CRL4 ubiquitin ligase. Lenalidomide can promote the expression of cleaved caspase-3, inhibit the expression of VEGF and induce apoptosis. |
| Target | Value |
| CRBN () | |
| VEGF () | |
| TNF-α (PBMCs) | 13 nM |
CAS:
191732-72-6
MF:
C13H13N3O3
MW:
259.26
EINECS:
691-297-1
MDL No.:
MFCD18064659
Melting point:
265-268 °C
Boiling point:
614.0±55.0 °C(Predicted)
Density
1.460±0.06 g/cm3(Predicted)
storage temp.
2-8°C
solubility
Soluble in DMSO (up to 30 mg/ml)
form
solid
pka
10.75±0.40(Predicted)
color
White
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
InChI
InChI=1S/C13H13N3O3/c14-9-3-1-2-7-8(9)6-16(13(7)19)10-4-5-11(17)15-12(10)18/h1-3,10H,4-6,14H2,(H,15,17,18)
InChIKey
GOTYRUGSSMKFNF-UHFFFAOYSA-N
SMILES
N1C(=O)CCC(N2CC3=C(C2=O)C=CC=C3N)C1=O
Xi'an Eastling biotech Co., Ltd. is dedicated to the research and development, production, and sales of natural plant extracts; With nearly 15 years of experience in identifying, researching, developing, and producing active ingredients for medicinal plants, we focus on providing innovative products and services to customers in industries such as pharmaceuticals, health food, and cosmetics.
Eastling Biotechnology has established a global direct harvesting system for plant raw materials, ensuring the high quality and authenticity of raw materials, while also protecting the continuity and diversity of plants; Having strong research and development capabilities, we can develop more effective and specialized plant active ingredients for the pharmaceutical, health food, and cosmetics industries; We have established an advanced quality control system, and the quality control of our products depends on advanced testing instruments and high-level technical experts. The effective combination of the two forms Eastling's ability to quickly and rigorously control product quality.
We have a production system that complies with Chinese GMP and American cGMP certifications, as well as advanced and optimized large-scale industrial production technology. In addition to producing specific products for Eastling Biotechnology, we also provide customized services to meet the characteristics and needs of different customers to produce customized products.
We believe that natural active ingredients are the foundation of our service to customers. Scientific and effective production technology is the foundation for us to provide customers with specialized products. We have the ability to serve customers in the pharmaceutical, health food, and cosmetics industries, provide new product solutions, and add new value to their products.