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

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

< td class="border-bottom: 1px dotted #ccc;padding: 5px;"> ARK5
(Cell-free assay)

Target	Value
TYK2 (Cell-free assay)	0.5 nM
MST1 (Cell-free assay)	4 nM
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

Cerdulatinib HCl salt(1369761-01-2)Related Product Information

• Pyridine hydrochloride
• 2'-Deoxyuridine
• Aniline hydrochloride
• Trimethylamine hydrochloride
• Betaine hydrochloride
• Methylamine hydrochloride
• Saracatinib
• 5-Azacytidine
• BIRB 796 (Doramapimod)
• 1-(4-(2-((4-chloro-2-hydroxy-5-iodophenyl)aMino)acetyl)piperazin-1-yl)prop-2-en-1-one
• Afatinib