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产品价格:电议      采购度:1615      原产地:美洲
发布时间:2021/7/24 0:26:50 所属地区:上海 上海市
简要描述:
Momelotinib (CYT387) 是 ATP 竞争性的 JAK1/JAK2 抑制剂,IC50 值分别为 11 nM/18 nM,是对 JAK3 选择性的 10 倍左右。
标签:CYT387
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CAS No. : 1056634-68-4
MCE 站:Momelotinib
产品活性:Momelotinib (CYT387) 是 ATP 竞争性的 JAK1/JAK2 抑制剂,IC50 值分别为 11 nM/18 nM,是对 JAK3 选择性的 10 倍左右。
研究领域:Epigenetics | Stem Cell/Wnt | JAK/STAT Signaling | Autophagy | Apoptosis
作用靶点:JAK | Autophagy | Apoptosis
In Vitro: Momelotinib (CYT387) inhibits the proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated by IL-3 with IC50 of 1400 nM. Furthermore, Momelotinib (CYT387) also causes the inhibition of cell proliferation in cell lines constitutively activated by JAK2 or MPL signaling, including Ba/F3-MPLW515L cells, CHRF-288-11 cells and Ba/F3-TEL-JAK2 cells with IC50 of 200 nM, 1 nM and 700 nM, respectively. In addition, Momelotinib (CYT387) has been shown to inhibit erythroid colony growth in vitro from JAK2V617F-positive PV patients with similar potency with IC50 of 2 μM-4 μM. Momelotinib (CYT387) inhibits PI3K/AKT and Ras/MAPK signaling induced by IL-6 and IGF-1. Moreover, Momelotinib (CYT387) induces apoptosis as a single agent and synergizes with the conventional anti-MM therapies PS-341 and L-PAM in primary multiple myeloma (MM) cells.
In Vivo: In a murine MPN model, Momelotinib (CYT387) normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Apoptosis Compound Library | Epigenetics Compound Library | Immunology/Inflammation Compound Library | JAK/STAT Compound Library | Kinase Inhibitor Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Differentiation Inducing Compound Library | Reprogramming Compound Library | Anti-COVID-19 Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | MG-132 | LY294002 | Doxorubicin hydrochloride | Bafilomycin A1 | Paclitaxel | Y-27632 dihydrochloride | Acetylcysteine | Angiotensin II human | SP600125 | 5-Fluorouracil | Staurosporine | Bortezomib | Tamoxifen | 2-Deoxy-D-glucose | Gemcitabine | Verteporfin | Decitabine | Actinomycin D | Temozolomide | BAY 11-7082 | Etoposide | Mitomycin C | CCCP | DAPT | Rotenone | Etomoxir | Stattic | Docetaxel | Fulvestrant
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更新时间:2024/1/2 10:14:29
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