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
