化合物Cerdulatinib hydrochloride T6104

Product Introduction
Bioactivity


英文名: Cerdulatinib hydrochloride

描述: Cerdulatinib hydrochloride (PRT2070 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，抑制 JAK1、2、3、SYK 和 Tyk2的 IC50值分别为12、6、8、32 和 0.5 nM。它可用于研究自身免疫性疾病和B 细胞恶性肿瘤。

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

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 40 mg/mL (83 mM)


关键字: 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

相关产品: Necrosulfonamide | GW806742X | IM-54 | AZ7550 | LY-364947 | URMC-099 | (E/Z)-Necrosulfonamide | MLKL-IN-2 | PRT062607 hydrochloride | AZ7550 trimesylate salt

相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Preclinical Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途