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7-(5-(1,5-dichloropentan-3-yl)-1-Methyl-1H-benzo[d]iMidazol-2-yl)-N-hydroxyheptanaMide

7-(5-(1,5-dichloropentan-3-yl)-1-Methyl-1H-benzo[d]iMidazol-2-yl)-N-hydroxyheptanaMide ??? ???
?? ??:
1236199-60-2
???:
7-(5-(1,5-dichloropentan-3-yl)-1-Methyl-1H-benzo[d]iMidazol-2-yl)-N-hydroxyheptanaMide
???(??):
CS-2555;EDO-S101;Minomustine;EDO-S101, 10 mM in DMSO;Tinostamustine(EDO-S101);EDO-S101;EDO S101;EDOS101;EDO-S101?(Tinostamustine);Histone deacetylases,Inhibitor,EDO-S101,EDOS101,inhibit,EDO S101,HDAC,EDO-S-101;1H-Benzimidazole-2-heptanamide, 5-[bis(2-chloroethyl)amino]-N-hydroxy-1-methyl-;7-{5-[bis(2-chloroethyl)amino]-1-methyl-1H-1,3-benzodiazol-2-yl}-N-hydroxyheptanamide
CBNumber:
CB62735711
???:
C19H28Cl2N4O2
??? ??:
415.36
MOL ??:
1236199-60-2.mol

7-(5-(1,5-dichloropentan-3-yl)-1-Methyl-1H-benzo[d]iMidazol-2-yl)-N-hydroxyheptanaMide ??

??
1.27±0.1 g/cm3(Predicted)
?? ??
under inert gas (nitrogen or Argon) at 2–8 °C
???
DMSO:14.0(Max Conc. mg/mL);33.71(Max Conc. mM)
Ethanol:2.0(Max Conc. mg/mL);4.82(Max Conc. mM)
??? ??
??? ??
?? ?? (pKa)
9.48±0.20(Predicted)
??
White to off-white

??

7-(5-(1,5-dichloropentan-3-yl)-1-Methyl-1H-benzo[d]iMidazol-2-yl)-N-hydroxyheptanaMide C??? ??, ??, ??

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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 ?? ?? ? ???

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7-(5-(1,5-dichloropentan-3-yl)-1-Methyl-1H-benzo[d]iMidazol-2-yl)-N-hydroxyheptanaMide ?? ??

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