Cerdulatinib HCl salt
Cerdulatinib HCl salt Basic information
- Product Name:
- Cerdulatinib HCl salt
- Synonyms:
-
- Cerdulatinib HCl salt
- 4-(cyclopropylamino)-2-[[4-[4-(ethylsulfonyl)-1-piperazinyl]phenyl]amino]-5-pyrimidinecarboxamide,hydrochloride (1:1)
- Cerdulatinib (PRT062070, PRT2070)
- Cerdulatinib HCl
- Cerdulatinib hydrochloride
- PRT062070 hydrochloride
- PRT2070 hydrochloride
- Cerdulatinib HCl salt USP/EP/BP
- CAS:
- 1369761-01-2
- MF:
- C20H28ClN7O3S
- MW:
- 481.99942
- Product Categories:
-
- Inhibitors
- Mol File:
- 1369761-01-2.mol
Cerdulatinib HCl salt Chemical Properties
- storage temp.
- under inert gas (nitrogen or Argon) at 2-8°C
- solubility
- DMSO:20.0(Max Conc. mg/mL);41.49(Max Conc. mM)
- form
- Solid
- color
- Light brown to brown
Cerdulatinib HCl salt Usage And Synthesis
Biological Activity
Cerdulatinib (PRT-062070, PRT2070) hydrochloride is an orally active multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 for JAK1/JAK2/JAK3/TYK2 and Syk, respectively nM and 32 nM. Also inhibits 19 other kinases tested with IC50s below 200 nM.
in vitro
Cerdulatinib affects BCR-mediated B cell activation through dual inhibition of SYK and JAK in human whole blood from normal donors. As a dual SYK/JAK inhibitor, Cerdulatinib significantly reduced cell viability in a subset of NHL cell lines and induced apoptosis in NHL cell lines with BCR signaling.
in vivo
In a rat collagen-induced arthritis model, Cerdulatinib (5 mg/kg po) significantly improved inflammatory infiltration of synovium and articular cartilage integrity. In addition, cerdulatinib also blocked BCR-induced B cell activation and splenomegaly in mice.
target
Target | Value |
TYK2 (Cell-free assay) | 0.5 nM |
MST1 (Cell-free assay) | 4 nM |
4 nM | |
MLK1 (Cell-free assay) td> | 5 nM |
Fms (Cell-free assay) | 5 nM |
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