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7-(5-(1,5-dichloropentan-3-yl)-1-Methyl-1H-benzo[d]iMidazol-2-yl)-N-hydroxyheptanaMide
- русский язык имя
- английское имя7-(5-(1,5-dichloropentan-3-yl)-1-Methyl-1H-benzo[d]iMidazol-2-yl)-N-hydroxyheptanaMide
- CAS №1236199-60-2
- CBNumberCB62735711
- ФормулаC19H28Cl2N4O2
- мольный вес415.36
- номер MDLMFCD29037367
- файл Mol1236199-60-2.mol
химическое свойство
плотность | 1.27±0.1 g/cm3(Predicted) |
температура хранения | under inert gas (nitrogen or Argon) at 2–8 °C |
растворимость | DMSO:14.0(Max Conc. mg/mL);33.71(Max Conc. mM) Ethanol:2.0(Max Conc. mg/mL);4.82(Max Conc. mM) |
форма | A crystalline solid |
пка | 9.48±0.20(Predicted) |
цвет | White to off-white |
FDA UNII | 29DKI2H2NY |
7-(5-(1,5-dichloropentan-3-yl)-1-Methyl-1H-benzo[d]iMidazol-2-yl)-N-hydroxyheptanaMide химические свойства, назначение, производство
Описание
EDO-S101 is a fusion molecule composed of the DNA alkylating agent bendamustine and the histone deacetylase (HDAC) inhibitor SAHA that inhibits class I and II HDACs (IC50s = 9-107 nM for HDAC1-3, 6, 8, and 10). It inhibits HDAC activity in rat peripheral blood mononuclear cells (PBMCs) ex vivo by 90% following a single dose of 10 mg/kg. EDO-S101 also induces formation of DNA crosslinks and double-strand breaks in HL-60 cells. It reduces growth of multiple myeloma (MM) cell lines irrespective of p53 mutational status or established resistance to DNA alkylating agents (IC50s = 1.6-4.8 μM). EDO-S101 also induces MM cell death ex vivo in bone marrow samples isolated from patients with early- and late-stage MM. In vivo, EDO-S101 (60 mg/kg per week) reduces tumor growth and prolongs survival in an MM1S end-stage mouse xenograft model. It also prolongs survival in a multidrug resistant Vk12653 mouse transplant model of refractory MM.7-(5-(1,5-dichloropentan-3-yl)-1-Methyl-1H-benzo[d]iMidazol-2-yl)-N-hydroxyheptanaMide поставщик
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