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Cerdulatinib HCl salt
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cerdulatinib HCl salt图片
CAS NO:1369761-01-2
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)482 (HCl salt)
FormulaC20H28ClN7O3S
CAS No.1369761-01-2 (HCl salt)
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 43 mg/mL (89.2 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo) 5% DMSO+corn oil: 3mg/mL
Synonyms

PRT062070; PRT 062070; PRT062070, PRT2070; PRT2070; PRT-2070; PRT 2070; PRT-06270

0Chemical Name: 4-(cyclopropylamino)-2-((4-(4-(ethylsulfonyl)piperazin-1-yl)phenyl)amino)pyrimidine-5-carboxamide hydrochloride

InChi Key: BGLPECHZZQDNCD-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H27N7O3S/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)

SMILES Code: O=C(C1=CN=C(NC2=CC=C(N3CCN(S(=O)(CC)=O)CC3)C=C2)N=C1NC4CC4)N

实验参考方法
In Vitro

In vitro activity: 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.


Kinase Assay: 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.


Cell Assay: 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.

In VivoIn 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.
Animal modelRat collagen-induced arthritis model
Formulation & DosageDissolved in 0.5% methylcellulose in water; 5 mg/kg; Oral administration
References

J Pharmacol Exp Ther. 2014 Dec;351(3):538-48.

生物活性


PRT062070 exhibits differential potency against cytokine JAK/STAT signaling pathways. J Pharmacol Exp Ther. 2014 Dec;351(3):538-48.



Dose responsive effect of PRT062070 in rat CIA treatment model. J Pharmacol Exp Ther. 2014 Dec;351(3):538-48.


PRT062070 blocks BCR-induced B-cell activation and splenomegaly in mice. J Pharmacol Exp Ther.2014 Dec;351(3):538-48.