| Identification | Back Directory | [Name]
Cerdulatinib HCl salt | [CAS]
1369761-01-2 | [Synonyms]
Cerdulatinib HCl
Cerdulatinib HCl salt
PRT2070 hydrochloride
PRT062070 hydrochloride
Cerdulatinib hydrochloride
Cerdulatinib HCl salt USP/EP/BP
Cerdulatinib (PRT062070, PRT2070)
4-(cyclopropylamino)-2-[[4-[4-(ethylsulfonyl)-1-piperazinyl]phenyl]amino]-5-pyrimidinecarboxamide,hydrochloride (1:1) | [Molecular Formula]
C20H28ClN7O3S | [MDL Number]
MFCD28348366 | [MOL File]
1369761-01-2.mol | [Molecular Weight]
481.999 |
| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,2-8°C | [solubility ]
DMSO:20.0(Max Conc. mg/mL);41.49(Max Conc. mM) | [form ]
Solid | [color ]
Light brown to brown |
| Hazard Information | Back Directory | [Uses]
Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC50s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies[1][2]. | [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 | < td style="border-bottom: 1px dotted #ccc;padding: 5px;"> ARK5
(Cell-free assay) 4 nM | MLK1
(Cell-free assay) | 5 nM | Fms
(Cell-free assay) | 5 nM |
| [IC 50]
Tyk2: 0.5 nM (IC50); JAK1: 12 nM (IC50); JAK2: 6 nM (IC50); JAK3: 8 nM (IC50); SYK: 32 nM (IC50); MST1: 4 nM (IC50); ARK5: 4 nM (IC50); MLK1: 5 nM (IC50); FMS: 5 nM (IC50); AMPK: 6 nM (IC50); TBK1: 10 nM (IC50); MARK1: 10 nM (IC50); PAR1B-a: 13 nM (IC50); TSSK: 14 nM (IC50); MST2: 15 nM (IC50); GCK: 18 nM (IC50); JNK3: 18 nM (IC50); Rsk2: 20 nM (IC50); Rsk4: 28 nM (IC50); CHK1: 42 nM (IC50); Flt4: 51 nM (IC50); Flt3: 90 nM (IC50); Ret: 105 nM (IC50); Itk: 194 nM (IC50) | [References]
[1] Coffey G, et al. The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. J Pharmacol Exp Ther. 2014 Dec; 351(3): 538-48. DOI:10.1124/jpet.114.218164
[2] Ishikawa C, et, al. Anti-adult T?cell leukemia/lymphoma activity of cerdulatinib, a dual SYK/JAK kinase inhibitor. Int J Oncol. 2018 Oct; 53(4): 1681-1690. DOI:10.3892/ijo.2018.4513 |
|
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
|