Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 249 | 现货 | ||
5 mg | ¥ 536 | 现货 | ||
10 mg | ¥ 715 | 现货 | ||
25 mg | ¥ 1,180 | 现货 | ||
50 mg | ¥ 1,790 | 现货 | ||
100 mg | ¥ 2,730 | 现货 | ||
500 mg | ¥ 6,290 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 568 | 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 | JAK2:6 nM, JAK1:12 nM, TYK2:0.5 nM, JAK3:8 nM, Syk:32 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 | Cerdulatinib, PRT2070, PRT062070 hydrochloride, PRT062070, PRT2070 hydrochloride |
分子量 | 482 |
分子式 | C20H28ClN7O3S |
CAS No. | 1369761-01-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0747 mL | 10.3734 mL | 20.7469 mL | 51.8672 mL |
5 mM | 0.4149 mL | 2.0747 mL | 4.1494 mL | 10.3734 mL | |
10 mM | 0.2075 mL | 1.0373 mL | 2.0747 mL | 5.1867 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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