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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。
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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 148 | 现货 | |
5 mg | ¥ 322 | 现货 | |
10 mg | ¥ 429 | 现货 | |
25 mg | ¥ 708 | 现货 | |
50 mg | ¥ 1,070 | 现货 | |
100 mg | ¥ 1,630 | 现货 | |
200 mg | ¥ 2,380 | 现货 |
产品描述 | 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. |
靶点活性 | JAK3:8 nM, Syk:32 nM, TYK2:0.5 nM, JAK1:12 nM, JAK2:6 nM |
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] |
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) |
别名 | PRT2070 hydrochloride, PRT2070, PRT062070 hydrochloride, PRT062070, Cerdulatinib |
分子量 | 482 |
分子式 | C20H28ClN7O3S |
CAS No. | 1369761-01-2 |
Smiles | Cl.CCS(=O)(=O)N1CCN(CC1)c1ccc(Nc2ncc(C(N)=O)c(NC3CC3)n2)cc1 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
溶解度信息 | 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. | ||||||||||||||||||||
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