化合物Cerdulatinib hydrochloride T6104
面议
- TargetMol
- 生产商
- 进口
- 美国
- 现货
- 全国
- 8
- 0
Product IntroductionBioactivity英文名: Cerdulatinib hydrochloride描述: Cerdulatinib hydrochloride (PRT2070 hydrochloride) 是一种选
AI问答
配套的仪器设备？
可以搭配的相关耗材试剂？
耗材描述
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
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
猜你喜欢
感兴趣产品