| CAS NO: | 1369761-01-2 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 482 (HCl salt) |
|---|---|
| Formula | C20H28ClN7O3S |
| 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 |
| 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 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. |
| Animal model | Rat collagen-induced arthritis model |
| Formulation & Dosage | Dissolved in 0.5% methylcellulose in water; 5 mg/kg; Oral administration |
| References | J Pharmacol Exp Ther. 2014 Dec;351(3):538-48. |
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. |
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