Cerdulatinib hydrochloride (PRT062070) 是一种选择性，具有口服活性和可逆的 ATP 竞争性的 SYK 和 JAK 的双重抑制剂，抑制 SYK 和 Tyk2、JAK1、2、3 的 IC₅₀ 值分别为 32 nM、0.5 nM、12 nM、6 nM 和 8 nM。Cerdulatinib hydrochloride 可用于研究自身免疫性疾病和B细胞恶性肿瘤。

Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC 50 s 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.

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Tyk2 0.5 nM (IC50) JAK1 12 nM (IC50

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.
Cerdulatinib (0.015-2 μM) inhibits FcεRI-mediated basophil degranulation with an IC50 of 0.12 μM.
Cerdulatinib (0.5-4 μM) exhibits differential potency against cytokine JAK/STAT signaling pathways.
Cerdulatinib (0-15 μM; 72 hours) results in viability effects similar to that of the combines SYK plus JAK-selective inhibition.
Cerdulatinib (1-3 μM; 48 hours) induces apoptosis in BCR-signaling competent non-Hodgkin lymphoma (NHL) cell lines. has not independently confirmed the accuracy of these methods.

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.
Cerdulatinib (?mg/kg; twice daily p.o. for 5 days) blocks BCR-induced B-cell activation and splenomegaly in mice. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.
[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.

In Vitro: DMSO : 20 mg/mL (41.49 mM; ultrasonic and warming and heat to 80°C)H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)配制储备液