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MedChemExpress - Model Cerdulatinib ...

MedChemExpress - Model Cerdulatinib hydrochloride - 1369761-01-2

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].

Cerdulatinib hydrochloride

MCE China：Cerdulatinib hydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-15999A

CAS：1369761-01-2

Synonyms：PRT062070 hydrochloride; PRT2070 hydrochloride

Purity：99.89%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：Cerdulatinib (0.03-4 μM) inhibits ERK Y204 phosphorylation with an IC50 of 0.5 μM and reduces the ability to upregulate cellsurface expression of the early activation marker CD69 with an IC50 of 0.11 μM in B cells in human whole blood[1]. Cerdulatinib (0.015-2 μM) inhibits FcεRI-mediated basophil degranulation with an IC50 of 0.12 μM[1]. Cerdulatinib (0.5-4 μM) exhibits differential potency against cytokine JAK/STAT signaling pathways[1]. Cerdulatinib (0-15 μM; 72 hours) results in viability effects similar to that of the combines SYK plus JAK-selective inhibition[1]. Cerdulatinib (1-3 μM; 48 hours) induces apoptosis in BCR-signaling competent non-Hodgkin lymphoma (NHL) cell lines[1].

In Vivo：Cerdulatinib (0.5-5 mg/kg; twice daily p.o. for 2 weeks) elicits dose-dependent efficacy in the rat collagen-induced arthritis (CIA) model[1]. Cerdulatinib ( mg/kg; twice daily p.o. for 5 days) blocks BCR-induced B-cell activation and splenomegaly in mice[1].

IC50 & Target：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. [Content Brief]

[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. [Content Brief]

Brand introduction:
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•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
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•   The biological activity of the products has been verified by the experiments of customers in various countries；
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