| 名称 | Cerdulatinib hydrochloride |
| 描述 | 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. |
| 细胞实验 | 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) |
| 激酶实验 | 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. |
| 体外活性 | 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] |
| 体内活性 | 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] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 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.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.07 mM), Sonication is recommended.
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| 关键字 | TyrosineKinases | Tyrosine Kinases | Tyk2 | Syk | PRT-2070 Hydrochloride | PRT-2070 | PRT-062070 Hydrochloride | PRT-062070 | PRT 2070 Hydrochloride | PRT 2070 | PRT 062070 Hydrochloride | PRT 062070 | MST1 | MLK1 | JAK | Hippopathway | Hippo pathway | dual | c-Fms | cFms | B-cell | autoimmune | ARK5 |
| 相关产品 | JAK-IN-10 | Tofacitinib Citrate | Gefitinib | Ruxolitinib | Raspberry ketone glucoside | Lentinan | Filgotinib | ANTHRAQUINONE-2-CARBOXYLIC ACID | Ellagic acid | Atinvicitinib | Ruxolitinib phosphate | Delgocitinib |
| 相关库 | 抑制剂库 | 经典已知活性库 | 抗癌活性化合物库 | 已知活性化合物库 | 临床失败化合物库 | 激酶抑制剂库 | 膜蛋白靶向化合物库 | 免疫/炎症分子化合物库 | 疼痛相关化合物库 | 药物功能重定位化合物库 | 酪氨酸激酶分子库 | 抗癌药物库 |