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EDO-S101
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EDO-S101
CAS No. : 1236199-60-2
MCE 站:EDO-S101
产品活性:EDO-S101 (Tinostamustine) 是 HDAC 的广谱抑制剂;抑制 HDAC1,HDAC2 和 HDAC3 的 IC50 值分别为 6 nM,9 nM,9 nM 和 25 nM。
研究领域:Cell Cycle/DNA Damage | Epigenetics
作用靶点:HDAC
In Vitro: EDOS101 inhibits HDAC activity in rat peripheral blood mononuclear cells (PBMCs) in a cellular assay by approximately 90% one hour after dosing with 10mg/kg i.v. HDAC inhibition in PBMCs could not be increased with higher doses up to 50mg/kg. EDO-S101 triggers apoptosis and shows strong antitumor activity in HL60 and Daudi cells. Initial in vitro experiments in HL60 cells shows an activation of the intrinsic pathway of apoptosis with cleavage of caspases 3, 9 and PARP and a marked reduction of anti-apoptotic proteins XIAP and Mcl-1.
In Vivo: Intracellular HDAC inhibition of EDO-S101, which occurs rapidly after dosing is at maximum activity already at the lowest dose of 10mg/kg and lasts for about 12-16 hours. Exposure to EDO-S101 causes a strong DNA repair response evidenced by activation of pH2AX and p53 in tumors taken from mice bearing subcutaneous human Burkitt’s lymphoma. Tumors of BL rapidly shrink or are completely eradicated after i.v. administration of EDO-S101.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Histone Modification Research Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Trichostatin A | 4-Phenylbutyric acid | Valproic acid | Entinostat | Sulforaphane | Romidepsin | RGFP966 | Tasquinimod | Corin | Tacedinaline | Dacinostat | ITSA-1 | SIS17 | Tubastatin A Hydrochloride | WT-161 | Givinostat hydrochloride monohydrate | Pyroxamide | BRD-6929 | Bufexamac | HDAC8-IN-1 | Scriptaid | Sinapinic acid | Apicidin | BML-210 | M344 | Droxinostat | HDACs/mTOR Inhibitor 1 | CG347B
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