型号:
产品价格:电议      采购度:1635      原产地:美洲
发布时间:2021/8/3 15:04:14 所属地区:上海 上海市
简要描述:
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。
标签:ASN-002
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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
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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更新时间:2024/1/2 10:17:44
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