An HDAC inhibitor and DNA alkylating agent; inhibits class I and II HDACs (IC50s = 9-107 nM for HDAC1-3

EDO-S101 – 1 mg

Brand:
Cayman
CAS:
1236199-60-2
Storage:
-20
UN-No:
Non-Hazardous - /

EDO-S101 is a fusion molecule composed of the DNA alkylating agent bendamustine and the histone deacetylase (HDAC) inhibitor SAHA (Item No. 10009929) that inhibits class I and II HDACs (IC50s = 9-107 nM for HDAC1-3, 6, 8, and 10).{38517} 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).{38518} 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.  

 

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Description

An HDAC inhibitor and DNA alkylating agent; inhibits class I and II HDACs (IC50s = 9-107 nM for HDAC1-3, 6, 8, and 10); inhibits HDAC activity in rat PBMCs ex vivo by 90% after a single dose of 10 mg/kg; induces formation of DNA crosslinks and double-strand breaks in HL-60 cells; reduces growth of MM cell lines irrespective of p53 mutational status or established resistance to DNA alkylating agents (IC50s = 1.6-4.8 μM); induces MM cell death ex vivo in bone marrow samples isolated from patients with early- and late-stage MM; reduces tumor growth and prolongs survival in an MM1S end-stage mouse xenograft model when administered at a dose of 60 mg/kg per week; prolongs survival in a multidrug resistant Vk12653 mouse transplant model of refractory MM,

Formal name: 5-[bis(2-chloroethyl)amino]-N-hydroxy-1-methyl-1H-benzimidazole-2-heptanamide

Synonyms: 

Molecular weight: 415.4

CAS: 1236199-60-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|DNA Alkylating Agents||Product Type|Biochemicals|Small Molecule Inhibitors|Deacetylases||Research Area|Cancer|Cell Death||Research Area|Cancer|DNA Damage and Repair|DNA Alkylating Agents||Research Area|Cancer|Multidrug Resistance

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