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Gusacitinib

CAS No. : 1425381-60-7

MCE 站：Gusacitinib

产品活性：Gusacitinib (ASN-002) 是一种有效的 SYK 激酶和 JAK 激酶的双抑制剂，IC₅₀ 值为 5-46 nM。Gusacitinib 在实体和血液肿瘤中均具有抗癌活性。

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

作用靶点：JAK  |  Syk

In Vitro: In mechanistic cell-based studies involving IgE and cytokine stimulations, Gusacitinib (ASN-002) strongly suppresses the SYK and JAK family kinase signaling pathways measured as pLAT and pSTAT levels, respectively. Gusacitinib (ASN-002) shows anti-proliferative activity in a broad panel of human cancer cell lines including DHL6, DHL4, OCI-LY10, H929, Pfeiffer, HT-1376, and Lovo, suggesting activity in both solid and hematological tumor types.

In Vivo: In a multiple myeloma (H929) xenograft model, Gusacitinib (ASN-002) exhibits significant efficacy in inhibiting tumor growth (>95%). It also significantly delays the onset of hind limb paralysis in the human erythroleukemia (HEL) mouse model. Gusacitinib (ASN-002) has good oral bioavailability, metabolic stability, is not a Pgp substrate, and shows little to no inhibition of CYP450 isozymes. Gusacitinib (ASN-002) shows a favorable safety profile in rat and dog toxicology studies.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  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  |  Clinical Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Anti-COVID-19 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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