Cerdulatinib hydrochloride 是一种选择性可逆，具有口服活性、 ATP 竞争性的Syk和JAK的双重抑制剂，它可用于研究自身免疫性疾病和B细胞恶性肿瘤。 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. 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) Information Cerdulatinib (PRT-062070, PRT2070) hydrochloride is an oral active, multi-targeted tyrosine kinase inhibitor withIC50of 12 nM/6 nM/8 nM/0.5 nM and 32 nM forJAK1/JAK2/JAK3/TYK2andSyk, respectively. Also inhibits 19 other tested kinases withIC50less than 200 nM. Targets TYK2 (Cell-free assay); MST1 (Cell-free assay); ARK5 (Cell-free assay); MLK1 (Cell-free assay); Fms (Cell-free assay);0.5 nM; 4 nM; 4 nM; 5 nM; 5 nM 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. 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. Cell Research(from reference) Cell lines：Ramos RA-1, Daudi, Toledo, SU-DHL4 and SU-DHL6 cells Concentrations：~15 μM Incubation Time：72 hours
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Cerdulatinib hydrochloride
CAS number：1369761-01-2 molecular formula：C20H28ClN7O3S
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| Chinese alias | - | ||
| English alias | 5-Pyrimidinecarboxamide, 4-(cyclopropylamino)-2-((4-(4-(ethylsulfonyl)-1-piperazinyl)phenyl)amino)-, hydrochloride (1:1) | 4-(cyclopropylamino)-2-((4-(4-(ethylsulfonyl)piperazin-1-yl)phenyl)amino)pyrimidine-5-carboxamide (hydrochloride) | Cerdulatinib HCl | ||
| CAS number | 1369761-01-2 | molecular formula | C20H28ClN7O3S |
| molecular weight | 482 g/mol | Exact mass | ≥98% |
| PSA | 142.000 Ų | logp | 1.862 |
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