Cerdulatinib NEW
| Price | $37 | $72 | $108 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: Cerdulatinib | CAS No.: 1198300-79-6 |
| Purity: 99.64% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | Cerdulatinib |
| Description | Cerdulatinib (PRT2070) is an novel oral dual Syk/JAK inhibitor. |
| Cell Research | Cerdulatinib is dissolved in DMSO. TMD8 cells are transfected with constructs of WT BTK or BTKC481S mutants using kit V, Program U-13 on Amaxa Nucleofector. After transfection, the cells are co-cultured with NKTert cells in a 24-well plate for 24 hrs for recovery. Ibrutinib, cerdulatinib and vehicle (DMSO) are then added into the transfected TMD8 cells and cellular viability is determined with MuseTM Count & Viability kit using Muse Cell Analyzer. The cell survival is determined by flow cytometry using the Annexin V/7-AAD Apoptosis Detection Kit I on freshly isolated CLL cells. |
| In vitro | Cerdulatinib effectively inhibits 60 CLL cells with IC50 values ranging between 0.37 to 10.02 μM, induces apoptosis via MCL-1 down-regulation and PARP cleavage, and overcomes microenvironmental support to trigger CLL cell death at 2 μM. It inhibits both ibrutinib-sensitive and -resistant primary CLL cell proliferation at concentrations of 250-500 nM, targets BTKC481S-transfected cell lines, halts BCR and JAK-STAT signaling, and blocks SYK and JAK leading to the downstream inhibition of AKT, ERK, and the NF-kB pathway. PRT062070, with an IC50 of 0.11 μM, limits stimulated B cell activation marker CD69 expression, demonstrating varied effectiveness against JAK/STAT pathways and induces apoptosis in BCR-signaling competent NHL cell lines at 1 or 3 μM. Cerdulatinib shows inhibitory actions on both ABC and GCB DLBCL cell subtypes, induces caspase 3 and PARP cleavage-mediated apoptosis, inhibits cell cycle progression through RB phosphorylation reduction and cyclin E down-regulation, and blocks JAK/STAT and BCR signaling. It elicits cell death in DLBCL cells under BCR stimulation and in primary human DLBCL samples, disrupts BCR-induced signaling, especially potent from 0.3 to 1 μM in IGHV-unmutated, high BCR signaling, sIgM, CD49d+, or ZAP70+ expressing samples, and neutralizes anti-IgM, IL4/CD40L, or NLC-mediated protection by preventing MCL-1 and BCL-XL upregulation, without affecting BCL-2 expression. Cerdulatinib also synergizes with venetoclax to enhance apoptosis in IL4/CD40L treated samples. |
| In vivo | Cerdulatinib (0.5 mg/kg) causes a nonstatistically significant trend toward reduced ankle inflammation, whereas significant reductions in inflammation are achieved with the 1.5, 3, and 5 mg/kg doses. Besides, Cerdulatinib also affects anticollagen antibody formation. Cerdulatinib (15 mg/kg) suppresses upregulation of splenic B-cell surface CD80/86 and CD69, and inhibits BCR signaling and activation in the spleen after oral dosing in mice[2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 40 mg/mL (89.78 mM), Sonication is recommended. |
| Keywords | Syk | Spleen tyrosine kinase | inhibit | JAK | PRT 2070 | PRT 062070 | Inhibitor | Cerdulatinib | Janus kinase | PRT-062070 | PRT-2070 |
| Inhibitors Related | ANTHRAQUINONE-2-CARBOXYLIC ACID | Ruxolitinib phosphate | Gefitinib |
| Related Compound Libraries | Bioactive Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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