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Cerdulatinib hydrochloride

CAS No. : 1369761-01-2

MCE 站：Cerdulatinib hydrochloride

产品活性：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。

研究领域：Protein Tyrosine Kinase/RTK  |  JAK/STAT Signaling  |  Epigenetics  |  Stem Cell/Wnt

作用靶点：Syk  |  JAK

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.
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.

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.
Cerdulatinib (?mg/kg; twice daily p.o. for 5 days) blocks BCR-induced B-cell activation and splenomegaly in mice.

相关产品：Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Stem Cell Signaling Compound Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Orally Active Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  AG490  |  Upadacitinib  |  AT9283  |  Piceatannol  |  Gandotinib  |  Lestaurtinib  |  Cucurbitacin I  |  Oclacitinib maleate  |  JANEX-1  |  BAY 61-3606 dihydrochloride  |  XL019  |  Atractylenolide I  |  FLLL32  |  LFM-A13  |  Brevilin A  |  ZM39923 hydrochloride  |  Ginsenoside Rk1  |  MNS  |  R112  |  WHI-P154  |  Curculigoside  |  FM-381  |  RO8191  |  Reticuline  |  Syk Inhibitor II  |  TCS 21311  |  WHI-P97  |  Syk-IN-1  |  Coumermycin A1

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