| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| C421401-1ml |
1ml |
现货  |
|
| 英文别名 | 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 |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | Cerdulatinib (PRT062070) hydrochloride |
| 生化机理 | Cerdulatinib（PRT-062070，PRT2070）盐酸盐是一种口服活性多靶点酪氨酸激酶抑制剂，对 JAK1/JAK2/JAK3/TYK2 和 Syk 的 IC50 分别为 12 nM/6 nM/8 nM/0.5 nM 和 32 nM。还能抑制 19 种其他受测激酶，IC50 小于 200 nM。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
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 |
| IC50 | JAK3, IC50: 8 nM |
|---|---|
| ALogP | 1.862 |
| hba_count | 5 |
| HBD Count | 3 |
| Rotatable Bond | 8 |
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| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IUPAC Name | 4-(cyclopropylamino)-2-[4-(4-ethylsulfonylpiperazin-1-yl)anilino]pyrimidine-5-carboxamide;hydrochloride |
| INCHI | InChI=1S/C20H27N7O3S.ClH/c1-2-31(29,30)27-11-9-26(10-12-27)16-7-5-15(6-8-16)24-20-22-13-17(18(21)28)19(25-20)23-14-3-4-14;/h5-8,13-14H,2-4,9-12H2,1H3,(H2,21,28)(H2,22,23,24,25);1H |
| InChi Key | IYULGYKOHUAYCG-UHFFFAOYSA-N |
| Canonical SMILES | CCS(=O)(=O)N1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C(C(=N3)NC4CC4)C(=O)N.Cl |
| Isomeric SMILES | CCS(=O)(=O)N1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C(C(=N3)NC4CC4)C(=O)N.Cl |
| 分子量 | 482 |
| Reaxy-Rn | 27631628 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=27631628&ln= |
| DMSO(mg / mL) Max Solubility | 43 |
|---|---|
| DMSO(mM) Max Solubility | 89.21161826 |
| Water(mg / mL) Max Solubility | ＜1 |
| 分子量 | 482.000 g/mol |
| XLogP3 | |
| 氢键供体数Hydrogen Bond Donor Count | 4 |
| 氢键受体数Hydrogen Bond Acceptor Count | 9 |
| 可旋转键计数Rotatable Bond Count | 8 |
| 精确质量Exact Mass | 481.166 Da |
| 单同位素质量Monoisotopic Mass | 481.166 Da |
| 拓扑极表面积Topological Polar Surface Area | 142.000 Ų |
| 重原子数Heavy Atom Count | 32 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 711.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 0 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 2 |
| Reaxy-Rn | 27631628 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=27631628&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
| 1. Zhihui Liao, Ning Pan, Jiale Liu, Chunyan Ma, Xue Xia, Jianju Deng, Guohui Yang, Xiaoan Li, Zhengguo Chen, Wencai Cheng, Wei Zhang, Xiaoqin Nie, Faqin Dong. (2024) Highly efficient iodide adsorption from medical radioactive wastewater by strong alkaline anion exchange fiber. Journal of Environmental Chemical Engineering, 12 (111783). [10.1016/j.jece.2023.111783] |
| 2. Jia Xu, Habib Khan, Li Yang. (2021) Hydrogel Paper-Based Analytical Devices: Separation-Free In Situ Assay of Small-Molecule Targets in Whole Blood. ANALYTICAL CHEMISTRY, 93 (44): (14755–14763). [PMID:34709797] [10.1021/acs.analchem.1c03347] |
| 1. Zhihui Liao, Ning Pan, Jiale Liu, Chunyan Ma, Xue Xia, Jianju Deng, Guohui Yang, Xiaoan Li, Zhengguo Chen, Wencai Cheng, Wei Zhang, Xiaoqin Nie, Faqin Dong. (2024) Highly efficient iodide adsorption from medical radioactive wastewater by strong alkaline anion exchange fiber. Journal of Environmental Chemical Engineering, 12 (111783). [10.1016/j.jece.2023.111783] |
| 2. Jia Xu, Habib Khan, Li Yang. (2021) Hydrogel Paper-Based Analytical Devices: Separation-Free In Situ Assay of Small-Molecule Targets in Whole Blood. ANALYTICAL CHEMISTRY, 93 (44): (14755–14763). [PMID:34709797] [10.1021/acs.analchem.1c03347] |
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