ChemicalBook > CAS DataBase List > 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

Product Name
7-(5-(1,5-dichloropentan-3-yl)-1-Methyl-1H-benzo[d]iMidazol-2-yl)-N-hydroxyheptanaMide
CAS No.
1236199-60-2
Chemical Name
7-(5-(1,5-dichloropentan-3-yl)-1-Methyl-1H-benzo[d]iMidazol-2-yl)-N-hydroxyheptanaMide
Synonyms
CS-2555;EDO-S101;Minomustine;EDO-S101, 10 mM in DMSO;Tinostamustine(EDO-S101);EDO-S101;EDO S101;EDOS101;EDO-S101?(Tinostamustine);Tinostamustine(EDO-S101) ，S8769;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-
CBNumber
CB62735711
Molecular Formula
C19H28Cl2N4O2
Formula Weight
415.36
MOL File
1236199-60-2.mol
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7-(5-(1,5-dichloropentan-3-yl)-1-Methyl-1H-benzo[d]iMidazol-2-yl)-N-hydroxyheptanaMide Property

Density 
1.27±0.1 g/cm3(Predicted)
storage temp. 
under inert gas (nitrogen or Argon) at 2–8 °C
solubility 
DMSO:14.0(Max Conc. mg/mL);33.71(Max Conc. mM)
Ethanol:2.0(Max Conc. mg/mL);4.82(Max Conc. mM)
form 
A crystalline solid
pka
9.48±0.20(Predicted)
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
23328
Product name
EDO-S101
Purity
≥98%
Packaging
1mg
Price
$81
Updated
2024/03/01
Cayman Chemical
Product number
23328
Product name
EDO-S101
Purity
≥98%
Packaging
5mg
Price
$356
Updated
2024/03/01
Cayman Chemical
Product number
23328
Product name
EDO-S101
Purity
≥98%
Packaging
10mg
Price
$632
Updated
2024/03/01
Cayman Chemical
Product number
23328
Product name
EDO-S101
Purity
≥98%
Packaging
25mg
Price
$1184
Updated
2024/03/01
AK Scientific
Product number
8336DG
Product name
Tinostamustine
Packaging
25mg
Price
$1416
Updated
2021/12/16
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7-(5-(1,5-dichloropentan-3-yl)-1-Methyl-1H-benzo[d]iMidazol-2-yl)-N-hydroxyheptanaMide Chemical Properties,Usage,Production

Description

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.

Uses

Tinostamustine (EDO-S101) is a pan HDAC inhibitor; inhibits HDAC6, HDAC1, HDAC2 and HDAC3 with IC50 values of 6 nM, 9 nM, 9 nM and 25 nM, respectively[1].

in vivo

Intracellular HDAC inhibition of Tinostamustine, 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 Tinostamustine 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 Tinostamustine[1].

IC 50

HDAC6: 6 nM (IC50); HDAC1: 9 nM (IC50); HDAC2: 9 nM (IC50); HDAC3: 25 nM (IC50); HDAC10: 72 nM (IC50); HDAC8: 107 nM (IC50)

References

[1] Mehrling T, et al. The Alkylating-HDAC Inhibition Fusion Principle: Taking Chemotherapy to the Next Level with the First in Class Molecule EDO-S101. Anticancer Agents Med Chem. 2016;16(1):20-8. DOI:10.2174/1871520615666150518092027

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

Raw materials

Preparation Products

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

China 56 United States 5 USA 1 Global 62
Acesys Pharmatech
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18860950986
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tangmanman@zenjipharma.com
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China
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Shanghai Lollane Biological Technology Co.,Ltd.
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021-52996696，15000506266 15000506266
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+86-21-52996696
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China
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Shanghai YuanYe Biotechnology Co., Ltd.
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021-61312847; 18021002903
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QQ:3008007432
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3008007409@qq.com
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China
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ShangHai Biochempartner Co.,Ltd
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177-54423994 17754423994
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Shanghai Rechem science Co., Ltd.
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Beijing Solarbio Science & Tecnology Co., Ltd.
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Beijing Jin Ming Biotechnology Co., Ltd.
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Chuzhou KeMail Chemical Technology Co., Ltd
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0550-5196001 15000891977
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Twochem Co.Ltd.
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021-58111628 15800915896
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QQ 3285589261
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Angel Pharmatech, Ltd.
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1236199-60-2, 7-(5-(1,5-dichloropentan-3-yl)-1-Methyl-1H-benzo[d]iMidazol-2-yl)-N-hydroxyheptanaMideRelated Search:


  • Tinostamustine(EDO-S101)
  • CS-2555
  • EDO-S101;EDO S101;EDOS101
  • 7-(5-(1,5-dichloropentan-3-yl)-1-Methyl-1H-benzo[d]iMidazol-2-yl)-N-hydroxyheptanaMide
  • EDO-S101
  • Minomustine
  • 7-{5-[bis(2-chloroethyl)amino]-1-methyl-1H-1,3-benzodiazol-2-yl}-N-hydroxyheptanamide
  • 7-(5-(bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)-N-hydroxyheptanamide
  • 1H-Benzimidazole-2-heptanamide, 5-[bis(2-chloroethyl)amino]-N-hydroxy-1-methyl-
  • Histone deacetylases,Inhibitor,EDO-S101,EDOS101,inhibit,EDO S101,HDAC,EDO-S-101
  • EDO-S101?(Tinostamustine)
  • EDO-S101, 10 mM in DMSO
  • Tinostamustine(EDO-S101) ，S8769
  • 1236199-60-2