CAS NO: | 1236199-60-2 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
生物活性 | EDO-S101 (Tinostamustine) is a panHDACinhibitor; inhibitsHDAC6,HDAC1,HDAC2andHDAC3withIC50values of 6 nM, 9 nM, 9 nM and 25 nM, respectively[1]. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (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. Initialin vitroexperiments 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[1]. | ||||||||||||||||
体内研究 (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[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 415.36 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C19H28Cl2N4O2 | ||||||||||||||||
CAS 号 | 1236199-60-2 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(240.76 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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