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Cerdulatinib 盐酸盐

JAK3 选择性抑制剂
2篇引用文献
  • ≥98%
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货号 (SKU) 包装规格 是否现货 价格 数量
C413796-10mg
 10mg 现货 Stock Image
C413796-50mg
 50mg 现货 Stock Image
C413796-100mg
 100mg 期货 Stock Image
大包装询价 添加到收藏夹 比较  SDS中文版  DATASHEET
查看相关系列
Histone Modification (1625) JAK (149) JAK/STAT Signaling (508) Non-receptor Tyrosine Kinase (795) Protein Tyrosine Kinase/RTK (1319) Stem Cell/Wnt (1019) Syk (36) 表观遗传学 (1497)
main product photo

基本描述

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 ≥98%
英文名称 Cerdulatinib 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 -20°C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 

产品属性

IC50 JAK3, IC50: 8 nM
ALogP 1.862
hba_count 5
HBD Count 3
Rotatable Bond 8

关联靶点（人）

STK26 Tchem 丝氨酸/苏氨酸蛋白激酶 26(Serine/threonine-protein kinase 26) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
BMP2K Tchem BMP-2诱导蛋白激酶(BMP-2-inducible protein kinase) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
Tchem 未表征蛋白 FLJ45252(Uncharacterized protein FLJ45252) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
AAK1 Tchem AP2 相关蛋白激酶 1(AP2-associated protein kinase 1) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EGFR Tclin Epidermal growth factor receptor erbB1 (33727 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
INSR Tclin Insulin receptor (5558 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TOP2A Tclin DNA topoisomerase II alpha (6317 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
IMPDH2 Tclin Inosine-5'-monophosphate dehydrogenase 2 (1326 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PDGFRB Tclin Platelet-derived growth factor receptor beta (5195 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
IGF1R Tclin Insulin-like growth factor I receptor (8605 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DCK Tchem Deoxycytidine kinase (530 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPK11 Tchem MAP kinase p38 beta (2785 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
LCK Tclin Tyrosine-protein kinase LCK (9212 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NQO2 Tchem Quinone reductase 2 (885 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPK14 Tchem MAP kinase p38 alpha (12866 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AK2 Tbio Adenylate kinase 2 (264 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKACB Tchem cAMP-dependent protein kinase beta-1 catalytic subunit (589 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKCZ Tchem Protein kinase C zeta (2414 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAP2K6 Tchem Dual specificity mitogen-activated protein kinase kinase 6 (1284 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MYLK Tchem Myosin light chain kinase, smooth muscle (1267 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1G1 Tchem Casein kinase I gamma 1 (2496 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FGFR1 Tclin Fibroblast growth factor receptor 1 (9149 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
STK3 Tchem Serine/threonine-protein kinase MST2 (3069 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKAG1 Tchem AMP-activated protein kinase, gamma-1 subunit (254 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAP2K5 Tchem Dual specificity mitogen-activated protein kinase kinase 5 (650 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SRC Tclin Tyrosine-protein kinase SRC (10310 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAP2K3 Tchem Dual specificity mitogen-activated protein kinase kinase 3 (632 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CDK6 Tclin Cyclin-dependent kinase 6 (1724 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKAG2 Tchem AMP-activated protein kinase, gamma-2 subunit (243 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AKT2 Tchem Serine/threonine-protein kinase AKT2 (4301 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AKT3 Tchem Serine/threonine-protein kinase AKT3 (3157 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GRK2 Tchem G-protein coupled receptor kinase 2 (1019 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PYGB Tchem Brain glycogen phosphorylase (474 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AURKB Tchem Serine/threonine-protein kinase Aurora-B (6805 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA4 Tchem Ribosomal protein S6 kinase alpha 4 (2104 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ROCK1 Tclin Rho-associated protein kinase 1 (4723 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIM1 Tchem Serine/threonine-protein kinase PIM1 (9629 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PKN2 Tchem Protein kinase N2 (1991 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSK Tchem Tyrosine-protein kinase CSK (2395 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA5 Tchem Ribosomal protein S6 kinase alpha 5 (3355 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKD3 Tchem Protein kinase C nu (2315 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKCI Tchem Protein kinase C iota (2821 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SYK Tclin Tyrosine-protein kinase SYK (7372 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
JAK1 Tclin Tyrosine-protein kinase JAK1 (8569 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA1 Tchem Ribosomal protein S6 kinase alpha 1 (2796 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA6 Tchem Ribosomal protein S6 kinase alpha 6 (2027 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PFKP Tbio Phosphofructokinase platelet type (224 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1E Tclin Casein kinase I epsilon (1412 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CAMK4 Tbio CaM kinase IV (2116 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3A Tclin Glycogen synthase kinase-3 alpha (3764 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKG1 Tchem cGMP-dependent protein kinase 1 beta (2814 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

Cdk4 Cyclin-dependent kinase 4 (3 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Pygl Liver glycogen phosphorylase (81 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Prkcd Protein kinase C delta (192 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Prkcb Protein kinase C beta (2 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mapk1 MAP kinase ERK2 (650 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Camk2g CaM kinase II gamma (1 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Tec Tyrosine-protein kinase TEC (25 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AIRC Multifunctional protein ADE2 (8 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Septin9 Septin-9 (1 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Acadvl Very long-chain specific acyl-CoA dehydrogenase, mitochondrial (1 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

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=

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 20 mg/mL warmed with 50ºC Water: bath (41.49 mM); Water: Insoluble; Ethanol: Insoluble;
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

安全和危险性（GHS）

Reaxy-Rn 27631628
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=27631628&ln=

 SDS英文版

技术规格说明书

Purity(HPLC area) 98-100（%）
NMR Spectrum 1H Conforms to structure
LC-MS for identification Conforms

 技术规格说明书

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批号(Lot Number) 证书类型 日期 货号
E2315958 分析证书 25-05-15 C413796
E23151004 分析证书 25-02-07 C413796
E23151089 分析证书 25-02-07 C413796

此产品的引用文献

如何在您的发表作品中引用阿拉丁的产品和网站?
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]

参考文献

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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