| Name | Cerdulatinib hydrochloride |
| Description | Cerdulatinib hydrochloride (PRT2070 hydrochloride) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM. |
| Cell Research | Cell lines (Ramos RA-1, Daudi, Toledo, SU-DHL4 and SU-DHL6) are cultured in RPMI media supplemented with 10% fetal bovine serum. Cells are treated with the indicated concentrations of PRT062070, the SYK-selective inhibitor PRT060318, the pan-JAK inhibitor 1, a 1:1 combination of PRT060318 and JAK inhibitor 1, or vehicle control (0.5% dimethylsulfoxide) for 72 hours. Cell viability assays are performed using CellTiter Glo in 384-well plates. Cells are seeded at a density of 5000 cells per well. (Only for Reference) |
| Kinase Assay | Purified Kinase Assays: Potency against purified SYK is determined by fluorescence resonance energy transfer. A broader panel of 270 purified kinases is surveyed in which PRT062070 is tested at a fixed concentration of 300 nM. [33P]-labeled substrate is measured after incubation of purified kinase with peptide substrate and [33P]ATP at the Km concentration for the kinase. |
| In vitro | In human whole blood from normal donors, Cerdulatinib affects BCR-mediated B-cell activation by dual inhibition of SYK and JAK. As a dual SYK/JAK inhibitor, Cerdulatinib significantly reduces cell viability in a subset of NHL cell lines, and induces apoptosis in BCR-signaling competent NHL cell lines. [1] |
| In vivo | In a rat collagen-induced arthritis model, Cerdulatinib (5 mg/kg p.o.) significantly improves inflammatory infiltrate within the synovium and the integrity of the articular cartilage. In addition, Cerdulatinib also blocks BCR-induced B-cell activation and splenomegaly in mice. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 4.82 mg/mL (10 mM), Sonication is recommended.
|
| Keywords | Inhibitor | malignancies | Tyk2 | PRT-2070 | PRT-062070 Hydrochloride | Cerdulatinib hydrochloride | PRT 062070 Hydrochloride | PRT-2070 Hydrochloride | PRT 2070 Hydrochloride | PRT062070 Hydrochloride | Janus kinase | PRT2070 Hydrochloride | JAK | Syk | Cerdulatinib Hydrochloride | autoimmune | dual | PRT 062070 | B-cell | PRT-062070 | Spleen tyrosine kinase | PRT 2070 | inhibit |
| Inhibitors Related | Delgocitinib | Deucravacitinib | Fedratinib | PLX5622 | Ruxolitinib | Tofacitinib Citrate | ANTHRAQUINONE-2-CARBOXYLIC ACID | Pexidartinib | Ibrutinib | Ruxolitinib phosphate | JAK-IN-10 | Gefitinib |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
